生物催化合成阿瑞吡坦关键手性中间体研究进展  

Research progress in biocatalytic synthesis of key chiral intermediate of Aprepitant

作　　者：欧阳斌[1] 何钰书 朱治任 王普[1] OUYANG Bin;HE Yushu;ZHU Zhiren;WANG Pu(College of Pharmaceutical Science,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：《发酵科技通讯》2018年第3期140-144,共5页Bulletin of Fermentation Science and Technology

基　　金：国家自然科学基金资助项目(21676250);浙江省自然科学基金资助项目(LY16B060010)

摘　　要：阿瑞吡坦是一种神经激肽-1(NK-1)受体阻断剂,是治疗癌症病人化疗型呕吐的药物,具有广阔的市场前景.(R)-3,5-双三氟甲基苯乙醇是合成阿瑞吡坦药物的关键手性中间体.利用生物催化法制备(R)-3,5-双三氟甲基苯乙醇具有立体选择性高、反应条件温和和环境友好等优点,近年来受到广泛关注.主要综述了生物不对称还原制备技术,包括酶催化、微生物细胞催化和重组工程菌催化,酶催化拆分制备技术,以及含离子液体新型介质体系中的微生物全细胞催化制备技术在(R)-3,5-双三氟甲基苯乙醇中的应用.Aprepitant, a neurokinin （NK 1） receptor antagonist, is mainly used for the treatment of chemotherapy induced nausea and vomiting in cancer patients with a wide range of market expectation. （R） [3, 5 his （trifluoromethyl） phenyl] ethanol is a key chiral intermediate of Aprepitant. In recent years, biosynthesis of （R） E3,5 bis（trifluoromethyl） phenyl] ethanol has attracted much attention due to its high stereoselectivity, mild reaction conditions and environmental friendly. In this paper, the research progress in biocatalytic synthesis of （R）-[3,5 bis（trifluoromethyl） phenyl] ethanol was summarized. The biotransformations performed in ionic liquid containing system were also introduced.

关 键 词：阿瑞吡坦 (R)-3 5-双三氟甲基苯乙醇 生物不对称还原 全细胞催化 

分 类 号：TQ46[化学工程—制药化工]