艾司佐匹克隆的拆分工艺研究  

Study on Enantioseparation of Eszopiclone

作　　者：赖群萍[1] 姜金娣[1] 张永江[1] 沈大冬[1] 

机构地区：[1]浙江医药股份有限公司新昌制药厂研究院,浙江新昌312500

出　　处：《精细化工中间体》2014年第3期45-48,共4页Fine Chemical Intermediates

摘　　要：以6-(5-氯-2-吡啶基)-5-羟基-7-氧代-6,7-二氢-5H-吡咯并[3,4-b]吡嗪为原料与4-甲基哌嗪-1-甲酰氯盐酸盐经过缩合得佐匹克隆、所得佐匹克隆经L-酒石酸拆分和重结晶得新型光谱纯镇静安眠药艾司佐匹克隆,目标化合物光学纯度大于99.7%,化学纯度大于99.5%。Eszopielone was obtained by the resolution of racemic zopiclone, which was synthesized by the reaction of 6-（5-chlorine-2-pyridinyl）-5-hydroxide-7-oxy-6,7-dihydrogen-5H-pyrrole[3,4-b]pyrazine with 4-methyl-1- piperazinecarbonyl chloride hydrochloride, with L-tartaric acid. The crude product was recrystallized from 95% ethanol affording e.e. of 99.7% and chemical purity of 99.5%.

关 键 词：镇静安眠药 艾司佐匹克隆 手性拆分 

分 类 号：R971.3[医药卫生—药品]