埃索美拉唑钠不对称氧化合成研究  

Study on Asymmetric Oxidation of Esomeprazole Sodium

作　　者：王智鹏 何佳钰 朱寒晓 龙雪 张洋[1] 

机构地区：[1]嘉兴学院生物与化学工程学院,浙江嘉兴314001

出　　处：《广州化工》2018年第3期81-83,共3页GuangZhou Chemical Industry

基　　金：嘉兴市科技局项目(2016AY13014);嘉兴学院校级重点SRT(SRT2017B054)

摘　　要：以D-(-)-酒石酸为手性源制备得到D-(-)-酒石酸四甲基铵手性离子液体,产品结构经~1H-NMR进行表征。在D-(-)-酒石酸四甲基铵作用下,配合催化剂钛酸四异丙酯及氧化剂进行埃索美拉唑的不对称氧化合成研究。结果表明,以与前手性硫醚等摩尔量的CHP为氧化剂、0.5摩尔当量的D-(-)-酒石酸四甲基铵为手性诱导剂、甲苯为反应溶剂、反应温度为25~30℃、反应时间为1.5 h为最优氧化工艺。D-(-)-tetramethylammonium tartrate prepared from D-(-)-tartaric acid was characterized by ~1 H-NMR. The asymmetric oxidation synthesis of esomeprazole was studied by using oxidant and titanium tetra-isopropoxide as catalyst,D-(-)-tetramethyl ammonium tartrate as inducer. The optimum oxidation process was as follows: CHP with equimolar amount of prochiral sulfide was used as oxidant,0. 5 mol equivalent of D-(-)-tetramethylammonium tartrate was used as chiral inducer,toluene was used as reaction solvent,the reaction temperature was 25 ~ 30 ℃,the reaction time was 1. 5 h.

关 键 词：D-(-)-酒石酸四甲基铵 埃索美拉唑 手性离子液体摇 

分 类 号：R914.5[医药卫生—药物化学]