C07C257/12

Method for preparing formamidines

A method for preparing formamidines of formula (I) in a single step by reducing ureas of formula (II) using silanes of formula (III), according to reaction (II)+(III)+(I) is provided. The present invention also provides a method for preparing insecticides, pesticides, fungicides, pharmaceutical products and catalysts, including a step of preparing formamidines of formula (I) according to the invention.

Method for preparing formamidines

A method for preparing formamidines of formula (I) in a single step by reducing ureas of formula (II) using silanes of formula (III), according to reaction (II)+(III)+(I) is provided. The present invention also provides a method for preparing insecticides, pesticides, fungicides, pharmaceutical products and catalysts, including a step of preparing formamidines of formula (I) according to the invention.

HIV REPLICATION INHIBITING PYRIMIDINES

This invention concerns HIV replication inhibitors of formula

##STR00001##

the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(O).sub.pR.sup.6, NHS(O).sub.pR.sup.6, C(O)R.sup.6, NHC(O)H, C(O)NHNH.sub.2, NHC(O)R.sup.6, C(NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, NN, O, C(O), C.sub.1-4alkanediyl, CHOH, S, S(O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(O)NHR.sup.13; C(O)NR.sup.13R.sup.14; C(O)R.sup.15; CHNNHC(O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

HIV REPLICATION INHIBITING PYRIMIDINES

This invention concerns HIV replication inhibitors of formula

##STR00001##

the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(O).sub.pR.sup.6, NHS(O).sub.pR.sup.6, C(O)R.sup.6, NHC(O)H, C(O)NHNH.sub.2, NHC(O)R.sup.6, C(NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, NN, O, C(O), C.sub.1-4alkanediyl, CHOH, S, S(O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(O)NHR.sup.13; C(O)NR.sup.13R.sup.14; C(O)R.sup.15; CHNNHC(O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

HIV replication inhibiting pyrimidines

This invention concerns HIV replication inhibitors of formula ##STR00001##
the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(O).sub.pR.sup.6, NHS(O).sub.pR.sup.6, C(O)R.sup.6, NHC(O)H, C(O)NHNH.sub.2, NHC(O)R.sup.6, C(NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, NN, O, C(O), C.sub.1-4alkanediyl, CHOH, S, S(O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(O)NHR.sup.13; C(O)NR.sup.13R.sup.14; C(O)R.sup.15; CHNNHC(O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

HIV replication inhibiting pyrimidines

This invention concerns HIV replication inhibitors of formula ##STR00001##
the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(O).sub.pR.sup.6, NHS(O).sub.pR.sup.6, C(O)R.sup.6, NHC(O)H, C(O)NHNH.sub.2, NHC(O)R.sup.6, C(NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, NN, O, C(O), C.sub.1-4alkanediyl, CHOH, S, S(O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(O)NHR.sup.13; C(O)NR.sup.13R.sup.14; C(O)R.sup.15; CHNNHC(O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

3-substituted phenylamidine compounds, preparation and use thereof

The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.4a, R.sup.4b, A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent. ##STR00001##

APPLICATION OF ADDITIVE, FORMAMIDINIUM IODIDE AND PREPARATION METHOD THEREFOR, PEROVSKITE SOLAR CELL, SOLAR POWER GENERATION APPARATUS, AND ELECTRICAL APPARATUS

An additive, formamidinium iodide and a preparation method therefor, a perovskite solar cell, a solar power generation apparatus, and an electrical apparatus. The additive includes a reducing agent. By incorporating the reducing agent in the additive and using the additive to prepare formamidinium iodide, generation of elemental iodine in the preparation process of formamidinium iodide can be reduced; in addition, iodine which has been oxidized to elemental iodine can be reduced to iodine anions so as to generate formamidinium iodide. The stability of formamidinium iodide is improved, and thus the stability and efficiency of perovskite cells are improved.

APPLICATION OF ADDITIVE, FORMAMIDINIUM IODIDE AND PREPARATION METHOD THEREFOR, PEROVSKITE SOLAR CELL, SOLAR POWER GENERATION APPARATUS, AND ELECTRICAL APPARATUS

An additive, formamidinium iodide and a preparation method therefor, a perovskite solar cell, a solar power generation apparatus, and an electrical apparatus. The additive includes a reducing agent. By incorporating the reducing agent in the additive and using the additive to prepare formamidinium iodide, generation of elemental iodine in the preparation process of formamidinium iodide can be reduced; in addition, iodine which has been oxidized to elemental iodine can be reduced to iodine anions so as to generate formamidinium iodide. The stability of formamidinium iodide is improved, and thus the stability and efficiency of perovskite cells are improved.