摘要
双(4-氟苯基)甲基酮(2)经还原,与氯化钠-浓硫酸氯代,再与哌嗪反应得1-[双(4-氟苯基)甲基]哌嗪(5),5在三氟乙酸为催化剂,三乙酰氧基硼氢化钠为还原剂的条件下和2,3,4-三甲氧基苯甲醛进行还原胺化得到洛美利嗪,然后成盐得盐酸洛美利嗪,总收率54%(以2计)。改进后的工艺更加绿色环保。
Lomerizine hydrochloride was prepared from bis （4-fluorophenyl）methanone（2） via reduction, chlorination with sodium chloride-concentrated sulfuric acid, reaction with piperazine to obtain the 1-[bis （4- fluorophenyl） methyl] piperazine （5）, which was subjected to reductive amination with 2,3,4-trimethoxybenzaldebyde with sodium triacetoxyborohydride as reducing agent and trifluoroacetic acid as catalyst, then salt formation with the overall yield of 54 % based on compound 2. The improved process was more friendly to environment.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第2期117-119,共3页
Chinese Journal of Pharmaceuticals
关键词
盐酸洛美利嗪
环保氯代
合成
还原胺化
lomerizine hydrochloride
green chlorination
synthesis
reductive amination
