申请人:The Upjohn Company
公开号:US04009175A1
公开(公告)日:1977-02-22
Compounds of the formula: ##STR1## wherein R'o and R"o are hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; R.sub.2 is phenyl, o-chlorophenyl, 0-fluorophenyl, 2,6-difluorophenyl and 2-pyridyl are prepared by multistep reactions from compounds of formula I: ##STR2## wherein R.sub.1 and R.sub.2 are defined as above and X is chlorine or bromine. Compounds of formula III, intermediates in the preparation thereof, Schiff's bases of compounds IIIA (III in which R'o and R"o are hydrogen), and the pharmacologically acceptable acid addition salts are useful in birds and mammals, including man, as sedatives, antianxiety, antidepressant, anticonvulsive, and muscular relaxing agents.
分子式为:##STR1## 其中R'o和R"o为氢或1至3个碳原子的烷基;R.sub.1为氢、氟、氯、溴、硝基、三氟甲基或烷基硫醚,其中烷基部分为1至3个碳原子;R.sub.2为苯基、邻氯苯基、邻氟苯基、2,6-二氟苯基和2-吡啶基,是由分子式I的化合物经多步反应制备而成:##STR2## 其中R.sub.1和R.sub.2如上所定义,X为氯或溴。分子式III的化合物,其制备中间体,化合物IIIA(III中R'o和R"o为氢的席夫碱)以及药理学上可接受的酸加成盐在鸟类和哺乳动物,包括人类中,可用作镇静剂、抗焦虑、抗抑郁、抗癫痫和肌肉松弛剂。