- Silver-Catalyzed C-H Trifluoromethylation of Arenes Using Trifluoroacetic Acid as the Trifluoromethylating Reagent
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Direct trifluoromethylation of arenes using TFA as the trifluoromethylating reagent was achieved with Ag as the catalyst. This reaction not only provides a new protocol for aryl C-H trifluoromethylation, but the generation of CF3· from TFA may prove useful in other contexts and could potentially be extended to other trifluoromethylation reactions. (Chemical Equation Presented).
- Shi, Guangfa,Shao, Changdong,Pan, Shulei,Yu, Jingxun,Zhang, Yanghui
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- Process for producing trifluoromethylbenzylamines
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The invention relates to a process for producing a trifluotomethylbenzylamine represented by the following general formula (1), 1where each R independently represents a halogen selected from the group consisting of fluorine, chlorine, bromine and iodine, an alkyl group having a carbon atom number of 1-4, an alkoxy group having a carbon atom number of 1-4, an amino group, a hydroxyl group or a trifluoromethyl group, and n represents an integer from 0 to 4. The process includes hydrogenating a trifluoromethylbenzonitrile by hydrogen in an organic solvent in the presence of ammonia and a catalyst containing a platinum group element. This trifluoromethylbenzonitrile is represented by the following general formula (2), 2where R and n are defined as above. With this process, it is possible to obtain the trifluoromethylbenzylamine at an extremely high yield.
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- Process for producing trifluoromethylbenzylamines
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The invention relates to a process for producing a trifluoromethylbenzylamine represented by the following general formula (1). This process includes hydrogenating a trifliuoromethylbenzonitrile represented by the following general formula (2) by hydrogen in an organic solvent in the presence of ammonia, using a Raney catalyst, where each R independently represents a halogen selected from the group consisting of fluorine, chlorine, bromine and iodine, an alkyl group having a carbon atom number of 1-4, an alkoxy group having a carbon atom number of 1-4, an amino group, a hydroxyl group or a trifluoromethyl group, and n represents an integer from 0 to 4, where R and n are defined as above. With this process, it is possible to obtain the trifluoromethylbenzylamine easily and inexpensively at an extremely high yield.
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- Antimycotically active substituted 2-aminothiazoles
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Antimicotically active 2-aminothiazoles have been found having the formula STR1 in which R1 represents hydrogen or alkyl and R2 represents optionally substituted cyclohexyl or phenyl which is substituted by halogen, alkyl, halogenoalkyl, halogenoalkoxy, dioxyhalogenoalkyl or halogenoalkylthio, and their physiologically tolerable acid addition salts, with the exception of the compounds 4-(4-chlorophenyl)-2-[2-(1,4,5,6-tetrahydropyrimidinyl)-amino]thiazole and 4-(2,4-dichlorophenyl)-2-[2-(1,4,5,6-tetrahydropyrimidinyl)-amino]-thiazole and 4-(4-chloro-2-methylphenyl)-2-[2-(1,4,5,6-tetrahydropyrimidinyl)-amino]-thiazole and with the exception of the physiologically tolerable acid addition salts of these compounds have been found.
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- Fluorine-containing acetophenones optionally halogenated on the CH3 -group and their precurser fluorine-containing benzonitriles
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Fluorine-containing acetophenones, optionally halogenated on the CH3 group, of the formula STR1 in which X represents hydrogen, chlorine or bromine and the radicals R1 to R5 have the following meaning, a) R1 and R4 denote fluorine, R2 and R5 denote chlorine and R3 denotes CF3, or b) R1, R3 and R4 denote fluorine and R2 and R5 denote hydrogen, or c) R1, R4 and R5 denote hydrogen, R2 denotes chlorine and R3 denotes CF3, or d) R1, R4 and R5 denote hydrogen, R2 denotes chlorine and R3 denotes OCF3, or e) R1, R4 and R5 denote hydrogen and R2 and R3 denote CF3, or f) R1 denotes chlorine, R2 denotes CF3 and R3, R4 and R5 denote hydrogen, or g) R1 denotes chlorine, R2, R3 and R4 denote hydrogen and R5 denotes CF3, or h) R1 denotes chlorine, R2, R4 and R5 denote hydrogen and R3 denotes CF3 and a process for their preparation from the corresponding fluorinated benzonitriles or benzyl halides by reaction with an organomagnesium compound capable of introducing methyl groups and subsequent hydrolysis, if appropriate followed by a chlorination or bromination.
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