摘要
以1-环丙基-6,7-二氟-8-甲氧基-4-氧代-1,4-二氢-3-喹啉羧酸乙酯为原料,用硼酸、醋酐进行螯合,再与(S,S)-2,8-二氮杂双环[4.3.0]壬烷进行缩合反应,在N,N-二甲基甲酰胺中与L-酒石酸成盐得酒石酸莫西沙星,最后在水中加入盐酸成盐得到莫西沙星成品。该方法反应条件温和,得到产品收率高,质量好,克服了其他文献报道工艺N-甲基莫西沙星杂质过大的问题。
Use ethyl 1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylate as raw material,react with boric acid and acetic anhydride,and then react with（4aS,7aS）-octahydro-1H pyrrolo [3,4-b] pyridine,and then react with L-（＋）-tartaric acid in DMF,finally in the water by adding hydrochloric acid to get moxifloxacin hydrochloride.The method has mild reaction condition,high yield and good quality is obtained,overcome the other reports in impurity of N-methyl moxifloxacin hydrochloride impurity is too large problem.
出处
《精细化工中间体》
CAS
2013年第1期33-36,62,共5页
Fine Chemical Intermediates
