两相体系中全细胞转化法制备托莫西汀中间体  

Preparation of Atomoxetine intermediate by whole cell transformation in phosphate buffer/organic solvent diphasic system

作　　者：欧志敏[1] 王莹[1] 泮佳莹 OU Zhimin;WANG Ying;PAN Jiaying(College of Pharmaceutical Sciences,Zhejiang University of Technology,Hangzhou 310014,China)

机构地区：[1]浙江工业大学药学院,浙江杭州310014

出　　处：《浙江工业大学学报》2018年第5期575-580,共6页Journal of Zhejiang University of Technology

基　　金：浙江省自然科学基金资助项目(LY15B060005)

摘　　要：研究了磷酸盐缓冲液/有机溶剂两相体系中,热带假丝酵母Candida tropicalis CGMCC NO.15016不对称还原3-羰基-3-苯基丙酸乙酯制备(R)-3-羟基-3-苯基丙酸乙酯的过程.利用二硝基水杨酸(DNS)法研究了有机溶剂对细胞的毒性,采用单因素法考察了相体积比、温度、磷酸盐缓冲液pH、底物浓度和菌体浓度等对不对称还原转化的影响,确定了V(磷酸盐缓冲液)∶V(邻苯二甲酸二丁酯两相体系)=1∶1为最佳反应体系,在最优转化条件下,转化率及对映体过剩值均可达到100%.(R)-3-hydroxy-3-ethyl phenylpropinate was synthesized by asymmetric reduction of 3-carbonyl-3-ethyl phenylpropinate with Candida tropicalis CGMCC NO.15016 as catalyst in phosphate buffer/organic solvent diphasic system.The DNS method was used to detect the toxicity of organic solvent to cells.The effects of different factors on the asymmetric reduction,such as the volume ratio of phosphate buffer to the organic phase,temperature,phosphate buffer pH,substrate concentration and cell concentration were investigated by single factor method.The conversion and enantiometric excess values can reach 100%in the optimum reaction system.

关 键 词：磷酸盐缓冲液/邻苯二甲酸二丁酯两相体系 热带假丝酵母 不对称还原 3-羰基-3-苯基丙酸乙酯 (R)-3-羟基-3-苯基丙酸乙酯 

分 类 号：R971.43[医药卫生—药品]