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    • 71. 发明授权
    • 6H-S-TRIAZOLO{8 4,3-a{9 {8 1,4{9 BENZODIAZEPIN-6-ONES
    • 6H-S-TRIAZOLO {8 4,3-a {9 {8 1,4 {9 BENZODIAZEPIN-6-ONES
    • US3870706A
    • 1975-03-11
    • US33526873
    • 1973-02-23
    • CIBA GEIGY CORP
    • ALLGEIER HANSGAGNEUX ANDRE
    • C07D243/14C07D487/04C07D53/06C07D55/06
    • C07D487/04
    • This invention provides a new process for the production of compounds of the class of 1-substituted 6-phenyl-4H-striazolo(4,3-a)(1,4)benzodiazepines and new intermediates for this process. The compounds produced by this process have valuable pharmacological properties. In particular, they possess anticonvulsant and antiaggressive activity and inhibit somatic reflexes. According to a specific embodiment, 1(benzyloxymethyl)4,5-dihydro-8-chloro-6H-s-triazolo(4,3a)(1,4)benzodiazepin-6-one is reacted with phenylmagnesium bromide, and the resulting 1-benzyloxymethyl)-6-phenyl-8-chloro4H-s-triazolo(4,3-a)(1,4)benzodiazepine is heated with hydrobromic acid-acetic acid to yield 6-phenyl-8-chloro-4H-striazolo(4,3-a)(1,4)benzodiazepine-1-methanol.
    • 本发明提供了一种用于生产1-取代的6-苯基-4H-s-三唑并[4,3-a] [1,4]苯并二氮杂类化合物的新方法和用于该方法的新中间体。 通过该方法制备的化合物具有有价值的药理学性质。 特别是它们具有抗惊厥和抗侵袭活性并抑制体细胞反射。 根据具体实施方案,使1-(苄氧基甲基)4,5-二氢-8-氯-6H-三唑并[4,3-a] [1,4]苯并二氮杂-6-酮与苯基溴化镁反应, 并将所得的1-苄氧基甲基)-6-苯基-8-氯-4H-三唑并[4,3-a] [1,4]苯并二氮杂环庚烷与氢溴酸 - 乙酸一起加热,得到6-苯基-8 [4,3-a] [1,4]苯并二氮杂-1-甲醇。