盐酸罗匹尼罗的合成  

Synthesis of Ropinirole Hydrochloride

作　　者：孙平华[1] 陈卫民[1] 李冰洲[1] 杨兆琪[1] 李茜[1] 

机构地区：[1]暨南大学药学院,广东广州510632

出　　处：《中国医药工业杂志》2007年第1期7-8,共2页Chinese Journal of Pharmaceuticals

摘　　要：2-甲基-3-硝基苯乙酸经氯代、酰胺化、还原得N,N-二丙基-2-甲基-3-硝基苯乙胺,与草酸二乙酯缩合、水解后还原得到2-硝基-6-[2-(二丙胺基)乙基]苯乙酸,最后经还原、缩合闭环及成盐反应制得盐酸罗匹尼罗,总收率约36%。Ropinirole hydrochlofide was synthesized from 2-methyl-3-nitrophenylacetic acid by chlorination, amidation, and reduction to give N,N-dipropyl-2-methyl-3-nitrophenethylamine, which was subjected to condensation with oxalic acid diethyl ester, hydrolysis and reduction to give 2-nitro-6-[2-（dipropylamino）ethyl] phenylacetic acid followed by reduction, cyclization and salt formation with an overall yield of about 36%.

关 键 词：罗匹尼罗 多巴胺D2受体激动剂 合成 

分 类 号：R972[医药卫生—药品]