Patent classifications
C07C231/14
4-(P-TRIFLUOROMETHYLBENZYL)-3-FLUORO-1,2,4-TRIPHENYLAMINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION AND APPLICATIONS THEREOF
A 4-(p-trifluoromethylbenzyl)-3-fluoro-1,2,4-triphenylamine derivative, a pharmaceutical composition and applications thereof are disclosed. The general chemical formula of the derivative is shown in formula I, where, R is a C.sub.1-C.sub.6 alkyl group, a cycloalkyl group, a heteroatom-containing cycloalkyl group, an aryl group or a heteroatom-containing aryl group, the heteroatom is selected from N or O, and the n is 0, 1, 2 or 3. The pharmaceutical composition contains any one of the above-mentioned 4-(p-trifluoromethylbenzyl)-3-fluoro-1,2,4-triphenylamine derivatives as an active ingredient, and one or more pharmaceutically acceptable carriers. The derivative and the pharmaceutical composition activate KCNQ channel currents. Thus, the derivative can be applied to prepare a KCNQ potassium channel opener, and can be used as the active ingredients of an antiepileptic pharmaceutical preparation, an antianxiety pharmaceutical preparation and a neuropathic pain-relieving pharmaceutical preparation.
A PROCESS METHOD FOR PRODUCING PESTICIDE BY USING CARBON DIOXIDE
A process method for producing pesticide by using carbon dioxide comprises the following steps: Weighing 1, 3-cyclohexanedione substrate, catalyst and Cs2CO3 in Schleck bottle, degassing, and continuously introducing 1 atm of carbon dioxide. Add solvent and react for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain 2(a-e). The obtained acid is acylated and then added dropwise to dichloromethane solution containing aniline to react for 2 h at normal temperature. After the reaction, column chromatography was performed to obtain 3(a-e). Add 3 (a-e) into 50% concentrated sulfuric acid and reflux at 80° C. for 8 hours. Through separation, 4(a-e) was obtained. The invention has the advantages that the catalyst is simple to prepare, has high catalytic activity, can be recycled, realizes industrial circulation, and achieves the goal of sustainable production. The preparation process of 3(a-e) and 4 (a-e) is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.
A PROCESS METHOD FOR PRODUCING PESTICIDE BY USING CARBON DIOXIDE
A process method for producing pesticide by using carbon dioxide comprises the following steps: Weighing 1, 3-cyclohexanedione substrate, catalyst and Cs2CO3 in Schleck bottle, degassing, and continuously introducing 1 atm of carbon dioxide. Add solvent and react for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain 2(a-e). The obtained acid is acylated and then added dropwise to dichloromethane solution containing aniline to react for 2 h at normal temperature. After the reaction, column chromatography was performed to obtain 3(a-e). Add 3 (a-e) into 50% concentrated sulfuric acid and reflux at 80° C. for 8 hours. Through separation, 4(a-e) was obtained. The invention has the advantages that the catalyst is simple to prepare, has high catalytic activity, can be recycled, realizes industrial circulation, and achieves the goal of sustainable production. The preparation process of 3(a-e) and 4 (a-e) is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.
METHODS OF MANUFACTURING 14,15-EPOXYEICOSATRIENOIC ACID ANALOGS AND IMPROVED THERAPEUTIC DELIVERY OF SAME
Systems, compositions, and methods are disclosed for developing and delivering therapeutically effective 14,15-epoxyeicosatrienoic acid (14,15-EET) analogs, for example for pain management or treatment. Of particular interest are intermediate salts.
METHODS OF MANUFACTURING 14,15-EPOXYEICOSATRIENOIC ACID ANALOGS AND IMPROVED THERAPEUTIC DELIVERY OF SAME
Systems, compositions, and methods are disclosed for developing and delivering therapeutically effective 14,15-epoxyeicosatrienoic acid (14,15-EET) analogs, for example for pain management or treatment. Of particular interest are intermediate salts.
CARBOXAMIDE AND SULFONAMIDE DERIVATIVES USEFUL AS TEAD MODULATORS
The invention is concerned with the compounds of formula (I) and formula (II):
##STR00001##
and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of using the compounds of formula (I) and formula (II) as well as pharmaceutical compositions containing such compounds. The compounds are useful in treating diseases and conditions mediated by TEAD, such as cancer.
CARBOXAMIDE AND SULFONAMIDE DERIVATIVES USEFUL AS TEAD MODULATORS
The invention is concerned with the compounds of formula (I) and formula (II):
##STR00001##
and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of using the compounds of formula (I) and formula (II) as well as pharmaceutical compositions containing such compounds. The compounds are useful in treating diseases and conditions mediated by TEAD, such as cancer.
METHOD AND MIXTURE TO FORM FUNCTIONALIZED CYCLIC COMPOUNDS
A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base:
##STR00001##
In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R.sup.2, G is an electron-withdrawing group, R.sup.1 is hydrogen or a substituent, and two of R.sup.1, R.sup.2 and G may joint together to form a ring. In formula (II), R.sup.3 and R.sup.4 are independently hydrogen or a substituent, R.sup.5 is an electron-withdrawing group, and two of R.sup.3, R.sup.4 and R.sup.5 may joint together to form a ring. The conjugate acid of the base has a pK.sub.a in the range of 1 to 15.
METHOD AND MIXTURE TO FORM FUNCTIONALIZED CYCLIC COMPOUNDS
A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base:
##STR00001##
In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R.sup.2, G is an electron-withdrawing group, R.sup.1 is hydrogen or a substituent, and two of R.sup.1, R.sup.2 and G may joint together to form a ring. In formula (II), R.sup.3 and R.sup.4 are independently hydrogen or a substituent, R.sup.5 is an electron-withdrawing group, and two of R.sup.3, R.sup.4 and R.sup.5 may joint together to form a ring. The conjugate acid of the base has a pK.sub.a in the range of 1 to 15.
ETHYLENEAMINE SULFONATE-BASED SURFACTANT FOR HIGH TEMPERATURE FOAMING
Surfactants constructed from three synthetic building blocks that contain multiple hydrocarbon chains, ethyleneamine, and alkyl sulfonate salt groups, were shown to possess good thermal stability, and foamability, and high foam profiles. The materials are targeted for high temperature foaming applications, such as foam flooding enhanced oil recovery to improve conformance control and other oil and gas downhole foaming applications.