FERROCENE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF

20220356199 · 2022-11-10

    Inventors

    Cpc classification

    International classification

    Abstract

    A ferrocene derivative has the formula (I), In formula (I), Z is selected from O, NH and S; R.sub.1 is selected from hydrogen, methyl and halogen; R.sub.2 is selected from hydrogen, halogen, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxy, C.sub.1-C.sub.6 haloalkyl, C.sub.1-C.sub.6 haloalkoxy and nitro; and n is an integer from 0 to 5, and R.sub.2 may be the same or different groups. The ferrocene derivative, a salt thereof, as well as a solvate thereof have anti-tumor activity, and can be used as candidate drugs or lead compounds for treating diseases such as tumor and cancer.

    ##STR00001##

    Claims

    1. A ferrocene derivative of formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof: ##STR00061## wherein Z is selected from NH, O and S; R.sub.1 is selected from hydrogen, C.sub.1-C.sub.6 alkyl and halogen; R.sub.2 is independently selected from hydrogen, halogen, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxy, C.sub.1-C.sub.6 haloalkoxy C.sub.1-C.sub.6 haloalkyl and nitro; and n is an integer from 0 to 5, and when n is greater than 1, R.sub.2 is selected from the same or different groups.

    2. The ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 1, wherein R.sub.1 is selected from hydrogen, methyl, chloro and fluoro, preferably, R.sub.2 is independently selected from at least one of the following groups: hydrogen, fluoro, chloro, bromo, methyl, ethyl, methoxy, trifluoromethyl, tert-butyl, cyano and nitro; and preferably, n is 1, 2 or 3.

    3. The ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 1, wherein the ferrocene derivative of formula (I) is any one of the following compounds: ##STR00062## ##STR00063## ##STR00064## ##STR00065## ##STR00066## ##STR00067## ##STR00068## ##STR00069## ##STR00070## ##STR00071## ##STR00072## ##STR00073## ##STR00074## ##STR00075## ##STR00076## ##STR00077## ##STR00078## ##STR00079## ##STR00080## ##STR00081## ##STR00082## ##STR00083## ##STR00084## ##STR00085## preferably, the pharmaceutically acceptable salt of the ferrocene derivative of formula (I) is a pharmaceutically acceptable salt formed by the compound of formula (I) with a pharmaceutically acceptable acid or a pharmaceutically acceptable cation; and preferably, the solvate includes hydrates and alcoholates.

    4. A preparation method for the ferrocene derivative of formula (I) according to claim 1, comprising the following steps: (1) reacting ferrocenylethyne with a compound of formula A to give a ferrocene-containing intermediate B; wherein the compound of formula A is 3-(R.sub.1)-4-bromobenzoic acid with a structural formula of ##STR00086## and the compound of formula B has a structural formula of ##STR00087## wherein R.sub.1 is defined as in claim 1; (2) reacting the intermediate B with a compound of formula C to give the ferrocene derivative of formula (I); ##STR00088## wherein the compound of formula C has a structural formula of wherein R.sub.2 and n are defined as in claim 1, and Z′ represents NH.sub.2, OH or SH;

    5. The preparation method according to claim 4, wherein the compound of formula C is 3-substituted phenyl-5-hydroxymethyl-isoxazole (II), 3-substituted phenyl-5-mercaptomethyl-isoxazole, or 3-substituted phenyl-5-aminomethyl-isoxazole (III), preferably, the reaction in step (1) is performed in the presence of a palladium(II) compound, an organophosphorus compound and a copper(I) compound; preferably, the reactions in step (1) and step (2) are performed in a dried organic solvent; preferably, the reaction in step (1) is also performed in the presence of an alkaline deacid reagent; preferably, the alkaline deacid reagent is selected from organic bases and/or inorganic bases, for example, the organic base is selected from one, two or more of triethylamine, tripropylamine, DMAP, DMF, N-methylmorpholine and the like; for example, the inorganic base is selected from one, two or more of potassium carbonate, sodium hydride, sodium carbonate and the like; preferably, step (1) comprises the following process: dispersing ferrocenylethyne and a compound of formula A in a mixture of a dried organic solvent and an alkaline deacid reagent, adding a palladium (II) compound, an organophosphorus compound and a copper (I) compound to the mixture while stirring, stirring the reaction system, refluxing the reaction system, filtering the reaction system, and concentrating the filtrate to give the intermediate B; and preferably, the reactions in step (1) and step (2) are performed under inert atmosphere.

    6. The preparation method according to claim 4, wherein the reaction in step (2) is performed in the presence of a condensing agent; for example, the condensing agent is selected from one, two or more of DCC, DMAP, NMM, HOBt and HATU; preferably, step (2) comprises the following process: adding the intermediate B to a dried organic solvent, then adding a condensing agent for reaction, followed by adding the compound of formula C for reaction to give the ferrocene derivative of formula (I); optionally, any functional group in the compound of formula C is protected; and optionally, the preparation method comprises removing any protecting agent.

    7. A pharmaceutical composition comprising the ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 1.

    8. A pharmaceutical preparation comprising the ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 1 preferably, the pharmaceutical preparation is a solid oral preparation, a liquid oral preparation or an injection.

    9. Use of the ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 1, or the pharmaceutical composition in the preparation of anti-tumor or anti-cancer drugs, wherein preferably, the tumor or cancer is selected from at least one of bladder cancer, ovarian cancer, breast cancer, gastric cancer, esophageal cancer, lung cancer, head and neck cancer, colon cancer, pharyngeal cancer and pancreatic cancer.

    10. Use of the ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 1 as an anti-tumor/anti-cancer lead compound, wherein preferably, the tumor or cancer is selected from at least one of bladder cancer, ovarian cancer, breast cancer, gastric cancer, esophageal cancer, lung cancer, head and neck cancer, colon cancer, pharyngeal cancer and pancreatic cancer.

    11. A pharmaceutical composition comprising the ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 2.

    12. A pharmaceutical composition comprising the ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 3.

    13. Use of the ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 2, or the pharmaceutical composition in the preparation of anti-tumor or anti-cancer drugs, wherein preferably, the tumor or cancer is selected from at least one of bladder cancer, ovarian cancer, breast cancer, gastric cancer, esophageal cancer, lung cancer, head and neck cancer, colon cancer, pharyngeal cancer and pancreatic cancer.

    14. Use of the ferrocene derivative of formula (I), the pharmaceutically acceptable salt thereof or the solvate thereof according to claim 3, or the pharmaceutical composition in the preparation of anti-tumor or anti-cancer drugs, wherein preferably, the tumor or cancer is selected from at least one of bladder cancer, ovarian cancer, breast cancer, gastric cancer, esophageal cancer, lung cancer, head and neck cancer, colon cancer, pharyngeal cancer and pancreatic cancer.

    Description

    DETAILED DESCRIPTION

    [0058] The present invention will be further illustrated with reference to the following examples. It should be noted that the following examples are not intended to limit the scope of the present invention, and any modifications made on the basis of the present invention do not depart from the spirit of the present invention.

    [0059] Among them, the synthesis of the intermediates and target compounds are all described in representative examples, and other intermediates and target compounds are synthesized in the same way as the synthesis of the representative compounds.

    [0060] Instruments and reagents:

    [0061] AVANCE III NMR spectrometer (400 MHz, DMSO-d6, TMS as internal standard), ion trap liquid chromatography-mass spectrometer (DECAX-30000 LCQ Deca XP), Shimadzu FTIR-84005 (manufactured by Shimadzu corporation, Japan), XT5 digital micro melting point apparatus (manufactured by Beijing Keyi Electric Optical Instrument Factory), and wavelength-tunable microplate reader (Molecular Devices SPECTRAMAX190).

    Example 1. Synthesis of Intermediates 3-substituted phenyl-5-hydroxymethyl-isoxazole (II) and 3-substituted phenyl-5-aminomethyl-isoxazole (III)

    [0062] With substituted benzaldehyde as the starting material, the compounds were prepared by oxime synthesis, 1,3-dipolar cycloaddition, methylsulfonyl esterification, azidation and reduction (R.sub.2 is selected from hydrogen, halogen, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxy, C.sub.1-C.sub.6 haloalkyl and nitro; n is an integer from 0 to 5), and the specific route was shown in the following figure:

    ##STR00032##

    [0063] Specific synthetic processes of the intermediates 3-substituted phenyl-5-hydroxymethyl-isoxazole (II) and 3-substituted phenyl-5-aminomethyl-isoxazole (III) are detailed in previous Chinese Patent Nos. CN103360382A, CN103664991A and CN103601762A by the applicant.

    Example 2. Synthesis of Ferrocene-Containing Intermediate B (Exemplified by the Synthesis with Ferrocenylethyne and p-bromobenzoic Acid):

    [0064] ##STR00033##

    [0065] Ferrocenylethyne (2.00 g, 9.52 mmol) and 4-bromobenzoic acid (1.91 g, 9.52 mmol) were added into a 250 mL two-necked round-bottom flask, and then dried tetrahydrofuran and triethylamine (60 mL) were added. The reaction system was stirred at room temperature for 10 min under nitrogen atmosphere. Then the reaction system was added with triphenylphosphine (0.2 g, 0.76 mmol), bis(triphenylphosphine)palladium chloride (0.28 g, 0.38 mmol) and copper(I) iodide (0.07 g, 0.38 mmol), stirred at room temperature for 20 min, and refluxed. The whole reaction was performed under nitrogen atmosphere. After the reaction system was completed, as detected by TLC, the reaction mixture was filtered, and the filtrate was concentrated to give a crude product, which was separated by column chromatography (V.sub.(petroleum ether): V.sub.(ethyl acetate)=5:1-1:1) to give 4-ferrocenylethynyl-benzoic acid (2.53 g, 81% yield) in the form of a light yellow solid. .sup.1H NMR of 4-ferrocenylethynyl-benzoic acid (400 MHz, DMSO-d.sub.6): 4.29 (s, 5H, η.sup.5-C.sub.5H.sub.5), 4.38 (2H, t, J=2.0 Hz), 4.61 (2H, t, J=2.0 Hz), 7.58 (2H, d, J=9.2 Hz), 7.90 (2H, d, J=9.2 Hz), 12.83 (1H, brs, —COOH).

    [0066] The other intermediates were prepared using 3-(R.sub.1)-4-bromobenzoic acid with R.sub.1 by referring to the reaction of ferrocenylethyne with 4-bromobenzoic acid.

    Example 3. Synthesis of the Target Ester Compound of Formula (I) (YJP-1)

    [0067] ##STR00034##

    [0068] 4-ferrocenylethynyl-benzoic acid prepared in Example 2 (0.165 g, 0.5 mmol) and dried THF (8 mL) were added to a 50 mL single-necked round-bottom flask, and then DCC (0.103 g, 0.5 mmol) and DMAP (0.061 g, 0.5 mmol) were added while stirring. The reaction system was reacted at 0° C. for 30 min. Then the reaction system was added with 3-phenyl-5-hydroxymethyl-isoxazole (0.088 g, 0.5 mmol), reacted at 0° C. for 30 min, and warmed to room temperature. The whole reaction was performed under nitrogen atmosphere. After the reaction was completed, as detected by TLC, the reaction solution was concentrated under reduced pressure, and the residue was separated by column chromatography (V.sub.(petroleum ether): V.sub.(ethyl acetate)=5:1-2:1) to give the target compound (YJP-1). The remaining compounds YJP-2 to YJP-76 were synthesized by referring to the synthesis process of the target compound YJP-1.

    Example 4. Synthesis of the Target Amide Compound of Formula (I) (YJP-77)

    [0069] ##STR00035##

    [0070] 4-ferrocenyl-benzoic acid prepared in Example 2 (0.165 g, 0.5 mmol) and dried THF (8 mL) were added to a 50 mL single-necked round-bottom flask, and then DCC (0.103 g, 0.5 mmol), HOBT (0.068 g, 0.5 mmol) and DMAP (0.061 g, 0.5 mmol) were added while stirring. The reaction system was reacted at 0° C. for 30 min. Then the reaction system was added with 3-phenyl-5-aminomethyl-isoxazole (0.087 g, 0.5 mmol), reacted at 0° C. for 30 min, and warmed to room temperature. The whole reaction was performed under nitrogen atmosphere. After the reaction was completed, as detected by TLC, the reaction solution was concentrated under reduced pressure, and the residue was separated by column chromatography (V.sub.(petroleum ether): V.sub.(ethyl acetate)=5:1-2:1) to give the target compound (YJP-77).

    [0071] The remaining compounds YJP-78 to YJP-152 were synthesized by referring to the synthesis process of the target compound YJP-77.

    ##STR00036## ##STR00037## ##STR00038## ##STR00039## ##STR00040## ##STR00041## ##STR00042## ##STR00043## ##STR00044## ##STR00045## ##STR00046## ##STR00047## ##STR00048## ##STR00049## ##STR00050## ##STR00051## ##STR00052## ##STR00053## ##STR00054## ##STR00055## ##STR00056## ##STR00057## ##STR00058## ##STR00059##

    [0072] The structures of the compounds YJP-1 to YJP-152 were all characterized by .sup.1H NMR analysis. The numbers and NMR data of the compounds YJP-1 to YJP-152 are shown in Table 1:

    ##STR00060##

    TABLE-US-00001 TABLE 1 .sup.1H NMR of the compounds of formula I No. R.sub.1 (R.sub.2).sub.n Z .sup.1H NMR (400 MHz, CDCl.sub.3) YJP-1 H H O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.48-7.52 (m, 3H, Ph—H), 7.83-7.85 (m, 2H, Ph—H), 7.59(d, 2H, J = 8.4 Hz), 8.09(d, 2H, J = 8.4 Hz). YJP-2 H 4-CH.sub.3 O 2.43(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C5H5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.31(d, 2H, J = 6.4 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.74(d, 2H, J = 8.0 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-3 H 4-CH.sub.2CH.sub.3 O 1.30(t, 3H, CH.sub.3, J = 7.6 Hz), 2.74(q, 2H, CH.sub.2CH.sub.3, J = 8.0 Hz), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.48(s, 2H), 6.71(s, 1H), 7.32(d, 2H, J = 8.0 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.76(d, 2H, J = 8.4 Hz), 8.07(d, 2H, J = 8.0 Hz). YJP-4 H 4-C(CH.sub.3).sub.3 O 1.38(s, 9H, 3CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.51(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.8 Hz), 7.79(d, 2H, J = 8.4 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-5 H 2,4,6-triCH.sub.3 O 2.18(s, 6H, 2CH.sub.3), 2.35(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.54(s, 2H), 6.36(s, 1H), 6.97(s, 1H), 7.29(s, 1H), 7.59(d, 2H, J = 8.4 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-6 H 4-OCH.sub.3 O 3.88(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.48(s, 2H), 6.68(s, 1H), 7.01(d, 2H, J = 7.2 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.79(d, 2H, J = 8.8 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-7 H 2-OCH.sub.3 O 3.94(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.50(s, 2H), 6.94(s, 1H), 7.02-7.09(m, 2H), 7.43-7.48(m, 1H), 7.57(d, 2H, J = 8.8 Hz), 7.93(dd, 1H, J = 1.6, 2.0 Hz), 8.06 (d, 2H, J = 8.4 Hz). YJP-8 H 3-OCH.sub.3 O 3.89(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.72(s, 1H), 7.01-7.04(m, 1H), 7.39-7.41(m, 1H), 7.58(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-9 H 4-F O 4.27(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.70(s, 1H), 7.18(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.8 Hz), 7.82(d, 2H, J = 8.8 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-10 H 2-F O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.87(s, 1H), 7.20-7.29(m, 3H), 7.44-7.49(m, 1H), 7.58(d, 2H, J = 8.8 Hz), 8.06(d, 2H, J = 8.8 Hz). YJP-11 H 4-Cl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.79(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-12 H 2-Cl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 6.90(s, 1H), 7.37-7.45(m, 2H), 7.53(dd, 1H, J = 1.2, 1.6 Hz), 7.58(d, 2H, J = 8.8 Hz), 7.76-7.79(m, 1H), 8.07(d, 2H, J = 8.4 Hz). YJP-13 H 2,4-diCl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.90(s, 1H), 7.38(dd, 1H, J = 2.0, 2.0 Hz), 7.55(d, 1H, J = 2.0 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.74(d, 1H, J = 8.4 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-14 H 4-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.79(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-15 H 2-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.86(s, 1H), 7.21(ddd, 1H, J = 0.8, 0.8, 1.2 Hz), 7.24(dd, 1H, J = 0.8, 1.2 Hz), 7.29(dd, 1H, J = 0.8, 1.2 Hz), 7.44-7.48(m, 1H), 7.55(d, 2H, J = 8.8 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-16 H 3-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 6.64(s, 1H), 7.69(d, 2H, J = 8.4 Hz), 7.63-7.68(m, 3H), 7.85(d, 1H, J = 7.6 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-17 H 4-CF.sub.3 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.52(s, 2H), 6.78(s, 1H), 7.58(d, 2H, J = 8.4 Hz), 7.76(d, 2H, J = 8.0 Hz), 7.98(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-18 H 2-CF.sub.3 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 6.64(s, 1H), 7.69(d, 2H, J = 8.4 Hz), 7.63-7.68(m, 3H), 7.85(d, 1H, J = 7.6 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-19 H 4-NO.sub.2 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 6.81(s, 1H), 7.45(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz), 8.36(d, 2H, J = 8.4 Hz). YJP-20 3′-CH.sub.3 H O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.48-7.52 (m, 3H, Ph—H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.83-7.85 (m, 2H, Ph—H). YJP-21 3′-CH.sub.3 4-CH.sub.3 O 2.43(s, 3H, CH.sub.3), 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.31(d, 2H, J = 6.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-22 3′-CH.sub.3 4-CH.sub.2CH.sub.3 O 1.30(t, 3H, CH.sub.3, J = 7.6 Hz), 2.49(s, 3H, CH.sub.3), 2.74(q, 2H, CH.sub.2CH.sub.3, J = 8.0 Hz), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.48(s, 2H), 6.71(s, 1H), 7.32(d, 2H, J = 8.0 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.76(d, 2H, J = 8.4 Hz). YJP-23 3′-CH.sub.3 4-C(CH.sub.3).sub.3 O 1.38(s, 9H, 3CH.sub.3), 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.51(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.79(d, 2H, J = 8.4 Hz). YJP-24 3′-CH.sub.3 2,4,6-TriCH.sub.3 O 2.18(s, 6H, 2CH.sub.3), 2.35(s, 3H, CH.sub.3), 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.54(s, 2H), 6.36(s, 1H), 6.97(s, 1H), 7.29(s, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-25 3′-CH.sub.3 4-OCH.sub.3 O 2.49(s, 3H, CH.sub.3), 3.88(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.48(s, 2H), 6.68(s, 1H), 7.01(d, 2H, J = 7.2 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.79(d, 2H, J = 8.8 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-26 3′-CH.sub.3 2-OCH.sub.3 O 2.49(s, 3H, CH.sub.3), 3.94(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.50(s, 2H), 6.94(s, 1H), 7.02-7.09(m, 2H), 7.43- 7.48(m, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.93(dd, 1H, J = 1.6, 2.0 Hz). YJP-27 3′-CH.sub.3 3-OCH.sub.3 O 2.49(s, 3H, CH.sub.3), 3.89(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.72(s, 1H), 7.01-7.04(m, 1H), 7.39- 7.41(m, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-28 3′-CH.sub.3 4-F O 2.49(s, 3H, CH.sub.3), 4.27(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.70(s, 1H), 7.18(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.83(d, 2H, J = 8.8 Hz). YJP-29 3′-CH.sub.3 2-F O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.87(s, 1H), 7.20-7.29(m, 3H), 7.44-7.49(m, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-30 3′-CH.sub.3 4-Cl O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.79(d, 2H, J = 8.4 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-31 3′-CH.sub.3 2-Cl O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 6.90(s, 1H), 7.37-7.45(m, 2H), 7.53(dd, 1H, J = 1.2, 1.6 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.76-7.79(m, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-32 3′-CH.sub.3 2,4-diCl O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.90(s, 1H), 7.38(dd, 1H, J = 2.0, 2.0 Hz), 7.55(d, 1H, J = 2.0 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.74(d, 1H, J = 8.4 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-33 3′-CH.sub.3 4-Br O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.79(d, 2H, J = 8.4 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-34 3′-CH.sub.3 2-Br O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.86(s, 1H), 7.21(ddd, 1H, J = 0.8, 0.8, 1.2 Hz), 7.24(dd, 1H, J = 0.8, 1.2 Hz), 7.29(dd, 1H, J = 0.8, 1.2 Hz), 7.44-7.48(m, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-35 3′-CH.sub.3 3-Br O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 6.64(s, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.63-7.68(m, 3H), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.85(d, 1H, J = 7.6 Hz). YJP-36 3′-CH.sub.3 4-CF.sub.3 O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.52(s, 2H), 6.78(s, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.76(d, 2H, J = 8.0 Hz), 7.85(d, 1H, J = 7.6 Hz), 7.98(d, 2H, J = 8.4 Hz). YJP-37 3′-CH.sub.3 2-CF.sub.3 O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 6.64(s, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.63-7.68(m, 3H), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.85(d, 1H, J = 7.6 Hz). YJP-38 3′-CH.sub.3 4-NO.sub.2 O 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 6.81(s, 1H), 7.45(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 8.36(d, 2H, J = 8.4 Hz). YJP-39 3′-Cl H O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.48-7.52 (m, 3H, Ph—H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.83-7.85 (m, 2H, Ph—H). YJP-40 3′-Cl 4-CH.sub.3 O 2.43(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.31(d, 2H, J = 6.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.74(d, 2H, J = 8.0 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-41 3′-Cl 4-CH.sub.2CH.sub.3 O 1.30(t, 3H, CH.sub.3, J = 7.6 Hz), 2.74(q, 2H, CH.sub.2CH.sub.3, J = 8.0 Hz), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.48(s, 2H), 6.71(s, 1H), 7.32(d, 2H, J = 8.0 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.76(d, 2H, J = 8.4 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-42 3′-Cl 4-C(CH.sub.3).sub.3 O 1.38(s, 9H, 3CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.51(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.81(d, 2H, J = 8.4 Hz). YJP-43 3′-Cl 2,4,6-TriCH.sub.3 O 2.18(s, 6H, 2CH.sub.3), 2.35(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.54(s, 2H), 6.36(s, 1H), 6.97(s, 1H), 7.29(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-44 3′-Cl 4-OCH.sub.3 O 3.88(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.48(s, 2H), 6.68(s, 1H), 7.01(d, 2H, J = 7.2 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.81(d, 2H, J = 8.8 Hz). YJP-45 3′-Cl 2-OCH.sub.3 O 3.94(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.50(s, 2H), 6.94(s, 1H), 7.02-7.09(m, 2H), 7.43-7.48(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.93(dd, 1H, J = 1.6, 2.0 Hz). YJP-46 3′-Cl 3-OCH.sub.3 O 3.89(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.72(s, 1H), 7.01-7.04(m, 1H), 7.39-7.41(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-47 3′-Cl 4-F O 4.27(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.70(s, 1H), 7.18(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.82(d, 2H, J = 8.8 Hz). YJP-48 3′-Cl 2-F O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.87(s, 1H), 7.20-7.29(m, 3H), 7.44-7.49(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-49 3′-Cl 4-Cl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.82(d, 2H, J = 8.4 Hz). YJP-50 3′-Cl 2-Cl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 6.90(s, 1H), 7.37-7.45(m, 2H), 7.53(dd, 1H, J = 1.2, 1.6 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.79-7.81(m, 1H). YJP-51 3′-Cl 2,4-DiCl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.90(s, 1H), 7.38(dd, 1H, J = 2.0, 2.0 Hz), 7.55(d, 1H, J = 2.0 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.74(d, 1H, J = 8.4 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-52 3′-Cl 4-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.79(d, 2H, J = 8.4 Hz). YJP-53 3′-Cl 2-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.86(s, 1H), 7.21(ddd, 1H, J = 0.8, 0.8, 1.2 Hz), 7.24(dd, 1H, J = 0.8, 1.2 Hz), 7.29(dd, 1H, J = 0.8, 1.2 Hz), 7.44-7.48(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-54 3′-Cl 3-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 6.64(s, 1H), 7.69(d, 2H, J = 8.4 Hz), 7.63-7.68(m, 3H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-55 3′-Cl 4-CF.sub.3 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.52(s, 2H), 6.78(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.76(d, 2H, J = 8.0 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.98(d, 2H, J = 8.4 Hz). YJP-56 3′-Cl 2-CF.sub.3 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 6.64(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.63-7.68(m, 3H), 7.78(d, 1H, J = 5.8 Hz), 7.85(d, 1H, J = 7.6 Hz). YJP-57 3′-Cl 4-NO.sub.2 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 6.81(s, 1H), 7.45(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 8.36(d, 2H, J = 8.4 Hz). YJP-58 3′-F H O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.48-7.52 (m, 3H, Ph—H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.83-7.85 (m, 2H, Ph—H). YJP-59 3′-F 4-CH.sub.3 O 2.43(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.3 1(d, 2H, J = 6.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.74(d, 2H, J = 8.0 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-60 3′-F 4-CH.sub.2CH.sub.3 O 1.30(t, 3H, CH.sub.3, J = 7.6 Hz), 2.74(q, 2H, CH.sub.2CH.sub.3, J = 8.0 Hz), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.48(s, 2H), 6.71(s, 1H), 7.32(d, 2H, J = 8.0 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.76(d, 2H, J = 8.4 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-61 3′-F 4-C(CH.sub.3).sub.3 O 1.38(s, 9H, 3CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 6.71(s, 1H), 7.51(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.81(d, 2H, J = 8.4 Hz). YJP-62 3′-F 2,4,6-TriCH.sub.3 O 2.18(s, 6H, 2CH.sub.3), 2.35(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.54(s, 2H), 6.36(s, 1H), 6.97(s, 1H), 7.29(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-63 3′-F 4-OCH.sub.3 O 3.88(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.48(s, 2H), 6.68(s, 1H), 7.01(d, 2H, J = 7.2 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.81(d, 2H, J = 8.8 Hz). YJP-64 3′-F 2-OCH.sub.3 O 3.94(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.50(s, 2H), 6.94(s, 1H), 7.02-7.09(m, 2H), 7.43-7.48(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.93(dd, 1H, J = 1.6, 2.0 Hz). YJP-65 3′-F 3-OCH.sub.3 O 3.89(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.72(s, 1H), 7.01-7.04(m, 1H), 7.39-7.41(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-66 3′-F 4-F O 4.27(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.70(s, 1H), 7.18(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.82(d, 2H, J = 8.8 Hz). YJP-67 3′-F 2-F O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.87(s, 1H), 7.20-7.29(m, 3H), 7.44-7.49(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-68 3′-F 4-Cl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.82(d, 2H, J = 8.4 Hz). YJP-69 3′-F 2-Cl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 6.90(s, 1H), 7.37-7.45(m, 2H), 7.53(dd, 1H, J = 1.2, 1.6 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.79-7.81(m, 1H). YJP-70 3′-F 2,4-DiCl O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.90(s, 1H), 7.38(dd, 1H, J = 2.0, 2.0 Hz), 7.55(d, 1H, J = 2.0 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.74(d, 1H, J = 8.4 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-71 3′-F 4-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.79(d, 2H, J = 8.4 Hz). YJP-72 3′-F 2-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 6.86(s, 1H), 7.21(ddd, 1H, J = 0.8, 0.8, 1.2 Hz), 7.24(dd, 1H, J = 0.8, 1.2 Hz), 7.29(dd, 1H, J = 0.8, 1.2 Hz), 7.44-7.48(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-73 3′-F 3-Br O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 6.64(s, 1H), 7.69(d, 2H, J = 8.4 Hz), 7.63-7.68(m, 3H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-74 3′-F 4-CF.sub.3 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.52(s, 2H), 6.78(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.76(d, 2H, J = 8.0 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.98(d, 2H, J = 8.4 Hz). YJP-75 3′-F 2-CF.sub.3 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 6.64(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.63-7.68(m, 3H), 7.78(d, 1H, J = 5.8 Hz), 7.85(d, 1H, J = 7.6 Hz). YJP-76 3′-F 4-NO.sub.2 O 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 6.81(s, 1H), 7.45(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 8.36(d, 2H, J = 8.4 Hz). YJP-77 H H NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.48-7.52 (m, 3H, Ph—H), 7.83-7.85 (m, 2H, Ph—H), 7.59(d, 2H, J = 8.4 Hz), 8.09(d, 2H, J = 8.4 Hz). YJP-78 H 4-CH.sub.3 NH 2.43(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.31(d, 2H, J = 6.4 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.74(d, 2H, J = 8.0 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-79 H 4-CH.sub.2CH.sub.3 NH 1.30(t, 3H, CH.sub.3, J = 7.6 Hz), 2.74(q, 2H, CH.sub.2CH.sub.3, J = 8.0 Hz), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.48(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.32(d, 2H, J = 8.0 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.76(d, 2H, J = 8.4 Hz), 8.07(d, 2H, J = 8.0 Hz). YJP-80 H 4-C(CH.sub.3).sub.3 NH 1.38(s, 9H, 3CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.51(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.8 Hz), 7.79(d, 2H, J = 8.4 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-81 H 2,4,6-TriCH.sub.3 NH 2.18(s, 6H, 2CH.sub.3), 2.35(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.54(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.36(s, 1H), 6.97(s, 1H), 7.29(s, 1H), 7.59(d, 2H, J = 8.4 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-82 H 4-OCH.sub.3 NH 3.88(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.48(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.68(s, 1H), 7.01(d, 2H, J = 7.2 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.79(d, 2H, J = 8.8 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-83 H 2-OCH.sub.3 NH 3.94(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.94(s, 1H), 7.02-7.09(m, 2H), 7.43-7.48(m, 1H), 7.57(d, 2H, J = 8.8 Hz), 7.93(dd, 1H, J = 1.6, 2.0 Hz), 8.06 (d, 2H, J = 8.4 Hz). YJP-84 H 3-OCH.sub.3 NH 3.89(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.72(s, 1H), 7.01-7.04(m, 1H), 7.39-7.41(m, 1H), 7.58(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-85 H 4-F NH 4.27(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.70(s, 1H), 7.18(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.8 Hz), 7.82(d, 2H, J = 8.8 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-86 H 2-F NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.87(s, 1H), 7.20-7.29(m, 3H), 7.44-7.49(m, 1H), 7.58(d, 2H, J = 8.8 Hz), 8.06(d, 2H, J = 8.8 Hz). YJP-87 H 4-Cl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.79(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-88 H 2-Cl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.90(s, 1H), 7.37-7.45(m, 2H), 7.53(dd, 1H, J = 1.2, 1.6 Hz), 7.58(d, 2H, J = 8.8 Hz), 7.76-7.79(m, 1H), 8.07(d, 2H, J = 8.4 Hz). YJP-89 H 2,4-DiCl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.90(s, 1H), 7.38(dd, 1H, J = 2.0, 2.0 Hz), 7.55(d, 1H, J = 2.0 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.74(d, 1H, J = 8.4 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-90 H 4-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.4 Hz), 7.79(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-91 H 2-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.86(s, 1H), 7.21(ddd, 1H, J = 0.8, 0.8, 1.2 Hz), 7.24(dd, 1H, J = 0.8, 1.2 Hz), 7.29(dd, 1H, J = 0.8, 1.2 Hz), 7.44- 7.48(m, 1H), 7.55(d, 2H, J = 8.8 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-92 H 3-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.64(s, 1H), 7.69(d, 2H, J = 8.4 Hz), 7.63-7.68(m, 3H), 7.85(d, 1H, J = 7.6 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-93 H 4-CF.sub.3 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.78(s, 1H), 7.58(d, 2H, J = 8.4 Hz), 7.76(d, 2H, J = 8.0 Hz), 7.98(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz). YJP-94 H 2-CF.sub.3 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.64(s, 1H), 7.69(d, 2H, J = 8.4 Hz), 7.63-7.68(m, 3H), 7.85(d, 1H, J = 7.6 Hz), 8.07(d, 2H, J = 8.4 Hz). YJP-95 H 4-NO.sub.2 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.81(s, 1H), 7.45(d, 2H, J = 8.4 Hz), 7.58(d, 2H, J = 8.4 Hz), 8.06(d, 2H, J = 8.4 Hz), 8.36(d, 2H, J = 8.4 Hz). YJP-96 3′-CH.sub.3 H NH 2.49(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.28(s, 5H, C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.48-7.52 (m, 3H, Ph—H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.83-7.85 (m, 2H, Ph—H). YJP-97 3′-CH.sub.3 4-CH.sub.3 NH 2.43(s, 3H, CH.sub.3), 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.31(d, 2H, J = 6.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-98 3′-CH.sub.3 4-CH.sub.2CH.sub.3 NH 1.30(t, 3H, CH.sub.3, J = 7.6 Hz), 2.49(s, 3H, CH.sub.3), 2.74(q, 2H, CH.sub.2CH.sub.3, J = 8.0 Hz), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.48(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.32(d, 2H, J = 8.0 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.76(d, 2H, J = 8.4 Hz). YJP-99 3′-CH.sub.3 4-C(CH.sub.3).sub.3 NH 1.38(s, 9H, 3CH.sub.3), 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.51(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.79(d, 2H, J = 8.4 Hz). YJP-100 3′-CH.sub.3 2,4,6-TriCH.sub.3 NH 2.18(s, 6H, 2CH.sub.3), 2.35(s, 3H, CH.sub.3), 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.54(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.36(s, 1H), 6.97(s, 1H), 7.29(s, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-101 3′-CH.sub.3 4-OCH.sub.3 NH 2.49(s, 3H, CH.sub.3), 3.88(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.48(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.68(s, 1H), 7.01(d, 2H, J = 7.2 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.79(d, 2H, J = 8.8 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-102 3′-CH.sub.3 2-OCH.sub.3 NH 2.49(s, 3H, CH.sub.3), 3.94(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.94(s, 1H), 7.02-7.09(m, 2H), 7.43-7.48(m, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.93(dd, 1H, J = 1.6, 2.0 Hz). YJP-103 3′-CH.sub.3 3-OCH.sub.3 NH 2.49(s, 3H, CH.sub.3), 3.89(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.72(s, 1H), 7.01-7.04(m, 1H), 7.39-7.41(m, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-104 3′-CH.sub.3 4-F NH 2.49(s, 3H, CH.sub.3), 4.27(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.70(s, 1H), 7.18(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.83(d, 2H, J = 8.8 Hz). YJP-105 3′-CH.sub.3 2-F NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.87(s, 1H), 7.20-7.29(m, 3H), 7.44-7.49(m, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-106 3′-CH.sub.3 4-Cl NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.79(d, 2H, J = 8.4 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-107 3′-CH.sub.3 2-Cl NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.90(s, 1H), 7.37-7.45(m, 2H), 7.53(dd, 1H, J = 1.2, 1.6 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.76-7.79(m, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-108 3′-CH.sub.3 2,4-DiCl NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.90(s, 1H), 7.38(dd, 1H, J = 2.0, 2.0 Hz), 7.55(d, 1H, J = 2.0 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.74(d, 1H, J = 8.4 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-109 3′-CH.sub.3 4-Br NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.79(d, 2H, J = 8.4 Hz), 7.82(d, 1H, J = 5.8 Hz). YJP-110 3′-CH.sub.3 2-Br NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.86(s, 1H), 7.21(ddd, 1H, J = 0.8, 0.8, 1.2 Hz), 7.24(dd, 1H, J = 0.8, 1.2 Hz), 7.29(dd, 1H, J = 0.8, 1.2 Hz), 7.44-7.48(m, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz). YJP-111 3′-CH.sub.3 3-Br NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.64(s, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.63-7.68(m, 3H), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.85(d, 1H, J = 7.6 Hz). YJP-112 3′-CH.sub.3 4-CF.sub.3 NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.78(s, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.76(d, 2H, J = 8.0 Hz), 7.85(d, 1H, J = 7.6 Hz), 7.98(d, 2H, J = 8.4 Hz). YJP-113 3′-CH.sub.3 2-CF.sub.3 NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.64(s, 1H), 7.58(d, 1H, J = 6.5 Hz), 7.63-7.68(m, 3H), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 7.85(d, 1H, J = 7.6 Hz). YJP-114 3′-CH.sub.3 4-NO.sub.2 NH 2.49(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.81(s, 1H), 7.45(d, 2H, J = 8.4 Hz), 7.58(d, 1H, J = 6.5 Hz), 7.72(s, 1H), 7.82(d, 1H, J = 5.8 Hz), 8.36(d, 2H, J = 8.4 Hz). YJP-115 3′-Cl H NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.48-7.52 (m, 3H, Ph—H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.83-7.85 (m, 2H, Ph—H). YJP-116 3′-Cl 4-CH.sub.3 NH 2.43(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.31(d, 2H, J = 6.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.74(d, 2H, J = 8.0 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-117 3′-Cl 4-CH.sub.2CH.sub.3 NH 1.30(t, 3H, CH.sub.3, J = 7.6 Hz), 2.74(q, 2H, CH.sub.2CH.sub.3, J = 8.0 Hz), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.48(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.32(d, 2H, J = 8.0 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.76(d, 2H, J = 8.4 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-118 3′-Cl 4-C(CH.sub.3).sub.3 NH 1.38(s, 9H, 3CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.51(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.81(d, 2H, J = 8.4 Hz). YJP-119 3′-Cl 2,4,6-TriCH.sub.3 NH 2.18(s, 6H, 2CH.sub.3), 2.35(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.54(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.36(s, 1H), 6.97(s, 1H), 7.29(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-120 3′-Cl 4-OCH.sub.3 NH 3.88(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.48(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.68(s, 1H), 7.01(d, 2H, J = 7.2 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.81(d, 2H, J = 8.8 Hz). YJP-121 3′-Cl 3-OCH.sub.3 NH 3.94(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.94(s, 1H), 7.02-7.09(m, 2H), 7.43-7.48(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.93(dd, 1H, J = 1.6, 2.0 Hz). YJP-122 3′-Cl 2-OCH.sub.3 NH 3.89(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.72(s, 1H), 7.01-7.04(m, 1H), 7.39-7.41(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-123 3′-Cl 4-F NH 4.27(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.70(s, 1H), 7.18(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.82(d, 2H, J = 8.8 Hz). YJP-124 3′-Cl 2-F NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.87(s, 1H), 7.20-7.29(m, 3H), 7.44-7.49(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-125 3′-Cl 4-Cl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.82(d, 2H, J = 8.4 Hz). YJP-126 3′-Cl 2-Cl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.90(s, 1H), 7.37-7.45(m, 2H), 7.53(dd, 1H, J = 1.2, 1.6 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.79-7.81(m, 1H). YJP-127 3′-Cl 2,4-DiCl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.90(s, 1H), 7.38(dd, 1H, J = 2.0, 2.0 Hz), 7.55(d, 1H, J = 2.0 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.74(d, 1H, J = 8.4 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-128 3′-Cl 4-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.79(d, 2H, J = 8.4 Hz). YJP-129 3′-Cl 2-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.86(s, 1H), 7.21(ddd, 1H, J = 0.8, 0.8, 1.2 Hz), 7.24(dd, 1H, J = 0.8, 1.2 Hz), 7.29(dd, 1H, J = 0.8, 1.2 Hz), 7.44- 7.48(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-130 3′-Cl 3-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.64(s, 1H), 7.69(d, 2H, J = 8.4 Hz), 7.63-7.68(m, 3H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-131 3′-Cl 4-CF.sub.3 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.78(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.76(d, 2H, J = 8.0 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.98(d, 2H, J = 8.4 Hz). YJP-132 3′-Cl 2-CF.sub.3 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.64(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.63- 7.68(m, 3H), 7.78(d, 1H, J = 5.8 Hz), 7.85(d, 1H, J = 7.6 Hz). YJP-133 3′-Cl 4-NO.sub.2 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.81(s, 1H), 7.45(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 8.36(d, 2H, J = 8.4 Hz). YJP-134 3′-F H NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.48-7.52 (m, 3H, Ph—H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.83-7.85 (m, 2H, Ph—H). YJP-135 3′-F 4-CH.sub.3 NH 2.43(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.31(d, 2H, J = 6.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.74(d, 2H, J = 8.0 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-136 3′-F 4-CH.sub.2CH.sub.3 NH 1.30(t, 3H, CH.sub.3, J = 7.6 Hz), 2.74(q, 2H, CH.sub.2CH.sub.3, J = 8.0 Hz), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.48(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.32(d, 2H, J = 8.0 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.76(d, 2H, J = 8.4 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-137 3′-F 4-C(CH.sub.3).sub.3 NH 1.38(s, 9H, 3CH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.51(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.81(d, 2H, J = 8.4 Hz). YJP-138 3′-F 2,4,6-TriCH.sub.3 NH 2.18(s, 6H, 2CH.sub.3), 2.35(s, 3H, CH.sub.3), 4.28(s, 5H, η.sup.5- C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.54(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.36(s, 1H), 6.97(s, 1H), 7.29(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-139 3′-F 4-OCH.sub.3 NH 3.88(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.48(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.68(s, 1H), 7.01(d, 2H, J = 7.2 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.81(d, 2H, J = 8.8 Hz). YJP-140 3′-F 2-OCH.sub.3 NH 3.94(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.50(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.94(s, 1H), 7.02-7.09(m, 2H), 7.43-7.48(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.93(dd, 1H, J = 1.6, 2.0 Hz). YJP-141 3′-F 3-OCH.sub.3 NH 3.89(s, 3H, OCH.sub.3), 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.72(s, 1H), 7.01-7.04(m, 1H), 7.39-7.41(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-142 3′-F 4-F NH 4.27(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.70(s, 1H), 7.18(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.82(d, 2H, J = 8.8 Hz). YJP-143 3′-F 2-F NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.87(s, 1H), 7.20-7.29(m, 3H), 7.44-7.49(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-144 3′-F 4-Cl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.82(d, 2H, J = 8.4 Hz). YJP-145 3′-F 2-Cl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.90(s, 1H), 7.37-7.45(m, 2H), 7.53(dd, 1H, J = 1.2, 1.6 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.79-7.81(m, 1H). YJP-146 3′-F 2,4-DiCl NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.90(s, 1H), 7.38(dd, 1H, J = 2.0, 2.0 Hz), 7.55(d, 1H, J = 2.0 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.74(d, 1H, J = 8.4 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-147 3′-F 4-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.51(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.71(s, 1H), 7.47(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.79(d, 2H, J = 8.4 Hz). YJP-148 3′-F 2-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.56(t, 2H, J = 2.0 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.86(s, 1H), 7.21(ddd, 1H, J = 0.8, 0.8, 1.2 Hz), 7.24(dd, 1H, J = 0.8, 1.2 Hz), 7.29(dd, 1H, J = 0.8, 1.2 Hz), 7.44- 7.48(m, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-149 3′-F 3-Br NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.64(s, 1H), 7.69(d, 2H, J = 8.4 Hz), 7.63-7.68(m, 3H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz). YJP-150 3′-F 4-CF.sub.3 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 1.6 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.52(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.78(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.76(d, 2H, J = 8.0 Hz), 7.78(d, 1H, J = 5.8 Hz), 7.98(d, 2H, J = 8.4 Hz). YJP-151 3′-F 2-CF.sub.3 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 1.6 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.64(s, 1H), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.63- 7.68(m, 3H), 7.78(d, 1H, J = 5.8 Hz), 7.85(d, 1H, J = 7.6 Hz). YJP-152 3′-F 4-NO.sub.2 NH 4.28(s, 5H, η.sup.5-C.sub.5H.sub.5), 4.31(t, 2H, J = 2.0 Hz), 4.55(t, 2H, J = 2.0 Hz), 5.53(s, 2H), 5.66(t, 1H, NH—CO—, J = 4.6 Hz), 6.81(s, 1H), 7.45(d, 2H, J = 8.4 Hz), 7.59(s, 1H), 7.68(d, 1H, J = 5.6 Hz), 7.78(d, 1H, J = 5.8 Hz), 8.36(d, 2H, J = 8.4 Hz).

    Example 5. In Vitro Anti-Tumor Activity Assay

    [0073] The compounds in the above examples were tested for in vitro anti-tumor activity using the CCK-8 method. The in vitro inhibitory activity of the compounds against breast cancer cell line (MCF-7), lung adenocarcinoma cell line (A549) and cervical cancer cell line (Hela) were mainly studied in this example. The breast cancer cell line (MCF-7), the lung adenocarcinoma cell line (A549) and the cervical cancer cell line (Hela) were obtained from cell lines stored in Ningxia Medical University. The specific test process was illustrated by the process for testing the breast cancer MCF-7 cell line: (1) Process for incubating breast cancer cell line (MCF-7) and testing inhibitory activities.

    [0074] The breast cancer cell line MCF-7 was incubated in an incubator for 24 h under the condition (37° C., 5% CO.sub.2, saturated humidity). When the cells were in logarithmic growth phase, the culture supernatant was removed, and the residue was digested with 0.25% trypsin-EDTA solution, and added with high glucose medium to terminate the digestion. The cells were seeded in a 96-well plate with a cell density of 5000 cells/well. The 96-well plate was incubated in an incubator for 24 h. Then the cell culture supernatant in the 96-well plate was removed. 100 μL of fresh high glucose medium was added to the 96-well plate, and samples at different concentrations were added to wells at 1 μL/well Subsequently, 1 μL solution of different concentrations were added to each well (every concentration was repeated for 5 times). After the plate was incubated for anothter 48 h at 37° C., 10 μL of CCK8 was added to each well, and the plate was then incubated at 37° C. for another 1-4 h. The absorbance of each well at 450 nm was measured on a multifunctional microplate reader. Inhibition rate%=[(OD.sub.control cells−OD.sub.treatment cells)/(OD.sub.control cells−OD.sub.blank)]×100. Negative control was a mixed solution of high glucose medium and DMSO at a ratio of V.sub.high lucose medium and V.sub.DMSO=10:1.

    [0075] (2) Process for incubating lung adenocarcinoma cell line (A549) and cervical cancer cell line (Hela) and testing inhibitory activities

    [0076] The experiment process for inhibiting the lung adenocarcinoma cell line (A549) and the cervical cancer cell line (Hela) was the same as the screening process of the breast cancer cell line (MCF-7). The results of activities of the preferred compounds for inhibiting breast cancer cell line MCF-7, human lung adenocarcinoma cell line A549 and cervical cancer cell line Hela are shown in the following Tables 2, 3 and 4 respectively.

    TABLE-US-00002 TABLE 2 Test results of the activities of some example compounds of formula (I) for inhibiting breast cancer cell line MCF-7 Compound no. Concentration (μM) Inhibition rate (%) YJP-2 14.37 85.39 YJP-3 10.68 91.74 YJP-4 10.68 94.48 YJP-6 16.05 77.46 YJP-7 16.63 57.41 YJP-8 19.34 80.48 YJP-14 16.22 86.13 YJP-18 11.35 88.12

    TABLE-US-00003 TABLE 3 Test results of the activities of some example compounds of formula (I) for inhibiting human lung adenocarcinoma cell line A549 Compound no. Concentration (μM) Inhibition rate (%) YJP-14 16.22 57.00 YJP-17 12.43 60.42 YJP-18 11.35 79.29

    TABLE-US-00004 TABLE 4 Test results of the activities of some example compounds of formula (I) for inhibiting cervical cancer cell line Hela Compound no. Concentration (μM) Inhibition rate (%) YJP-4 10.68 60.10 YJP-13 9.91 74.80 YJP-14 16.22 68.26 YJP-17 12.43 57.62 YJP-18 11.35 63.99 YJP-19 10.53 88.94

    [0077] The examples of the present invention have been described above. However, the present invention is not limited to the above examples. Any modification, equivalent, improvement and the like made without departing from the spirit and principle of the present invention shall fall within the protection scope of the present invention.