莫西沙星手性侧链的合成  

The Synthesis of Moxifloxacin Chiral Sidechain

作　　者：崔栋[1] 范铮[1] 刘加庚[2] 

机构地区：[1]浙江工业大学,浙江杭州310014 [2]浙江大学化学系,浙江杭州310028

出　　处：《浙江化工》2013年第8期5-9,共5页Zhejiang Chemical Industry

摘　　要：莫西沙星是第四代氟喹诺酮类药物,临床应用领域广、效果良好,市场潜力巨大。传统生产工艺中由于其侧链都要进行手性拆分,因此目前其生产成本主要来于此侧链的合成。本研究以具有手性的D-苯甘氨醇为原料,经过两步成环、双键和羰基的还原、开环及酸化直接制得具有手性的二酸中间体,再经过上苄基、羰基还原及脱苄,制得终产物(S,S)-2,8-二氮杂双环[4.3.0]壬烷,总收率达到35.2%,成功完成了一条莫西沙星手性侧链的合成路线。Moxifloxacin is a fourth-generation fluoroquinolones. It has wide clinical applications, good effect and huge market potential. The sidechain should be carried out chiral separation in traditional production process, so this led to high production costs. （S,S）-2,8-diazabicyclo[4.3.0]nonane was synthesized from D-phenylglycinol by two steps into the ring, reduction of double bond and carbonyl group, open-loop and acidification, benzyl protecting, earbonyl reduction and debenzylation with an overall yield of 35.2%.

关 键 词：莫西沙星侧链 (S S)-2 8-二氮杂双环[4 3 0]壬烷 合成路线 

分 类 号：TQ463[化学工程—制药化工]