首页> 外国专利> 7-BROMO-1,2-METHYLENE-5- (2-HALOGENPHENYL) -1H-2,3-DIHYDRO-1,4-BENZODIAZEPINES AND PROCEDURE FOR THE PREPARATION OF 7-BROM-5- (2-HALOGENPHENYL) -1H- 2,3-DIHYDRO-1,4-BENZODIAZEPINE COMPOUNDS OR ACID ADDITION SALTS THEREOF

7-BROMO-1,2-METHYLENE-5- (2-HALOGENPHENYL) -1H-2,3-DIHYDRO-1,4-BENZODIAZEPINES AND PROCEDURE FOR THE PREPARATION OF 7-BROM-5- (2-HALOGENPHENYL) -1H- 2,3-DIHYDRO-1,4-BENZODIAZEPINE COMPOUNDS OR ACID ADDITION SALTS THEREOF

机译:7-溴-1,2-亚甲基-5-(2-卤代苯基)-1H-2,3-二氢-1,4-苯并二氮杂AND和制备7-溴-5-(2-卤代苯基)-1H的方法-2,3-二氢-1,4-苯二氮杂化合物或其酸附加盐

摘要

Disclosed are 7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines of the formula I IMAGE I in which R1 is a hydrogen atom or a lower alkoxy or alkanoyloxy radical and R2 is a halogen atom. The compounds possess psychopharmacological, and especially anti-aggressive properties. To manufacture compounds of formula I, corresponding 2-halomethyl-7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines are cyclized to corresponding 7-bromo-1,2-methylene-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines and in these the aziridine ring is opened through treatment with a lower alcohol or a lower carboxylic acid in the presence of a Lewis acid.
机译:公开了式I I的7-溴-5-(2-卤代苯基)-1H-2,3-二氢-1,4-苯并二氮杂s其中R1为氢原子或低级烷氧基或烷酰氧基的基团,并且R 2是卤素原子。这些化合物具有心理药理学特性,尤其是具有抗攻击性。为了制备式I的化合物,将相应的2-卤甲基-7-溴-5-(2-卤苯基)-1H-2,3-二氢-1,4-苯并二氮杂环化成相应的7-溴-1,2-亚甲基-5-(2-卤代苯基)-1H-2,3-二氢-1,4-苯并二氮杂and,其中氮丙啶环通过在路易斯酸存在下用低级醇或低级羧酸处理而打开。

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