申请人:The Upjohn Company
公开号:US04028356A1
公开(公告)日:1977-06-07
Compounds of formula IV: ##STR1## wherein R and R.sub.2 are hydrogen or methyl; wherein R.sub.1 is --COOH, --COOR' in which R' is alkyl of 1 to 3 carbon atoms, inclusive, --(CnH.sub.2 n)A in which n is an integer of 1 to 3 and A is fluoro, chloro, bromo, trifluoromethyl, hydroxy, alkoxy, in which the alkyl group is defined as above, or ##STR2## in which R" and R'" are hydrogen or alkyl as defined above or together ##STR3## is pyrrolidino, piperidino, morpholino, 4-methylpiperazino, 4-(2-hydroxyethyl)-piperazino; wherein R.sub.3 is hydrogen, fluoro, chloro, bromo, trifluoromethyl, or nitro; and wherein Ar is phenyl, o-chlorophenyl, o-fluorophenyl, 2,6-difluorophenyl, or 2-pyridyl, are produced. The compounds of formula IV of this invention are sedatives, tranquilizers and muscle-relaxants and can be used for such purposes in mammals and birds.
IV式化合物:##
STR1##其中R和R.sub.2为
氢或
甲基;其中R.sub.1为--COOH,--COOR',其中R'为1至3个
碳原子的烷基,包括,--(CnH.sub.2 n)A,其中n为1至3的整数,A为
氟、
氯、
溴、三
氟甲基、羟基、烷
氧基,其中烷基团如上所定义,或##
STR2##其中R"和R'"为如上所定义的
氢或烷基,或一起##
STR3##为
吡咯啉基、
哌啶基、
吗啉基、4-
甲基哌嗪基、4-(2-羟乙基)-
哌嗪基;其中R.sub.3为
氢、
氟、
氯、
溴、三
氟甲基或硝基;Ar为
苯基、邻
氯苯基、邻
氟苯基、
2,6-二氟苯基或2-
吡啶基。本发明的IV式化合物是镇静剂、
安定剂和肌肉松弛剂,可用于哺乳动物和鸟类。