克唑替尼药物关键手性中间体合成进展  

Research Progress in Synthesis of a Key Chiral Intermediate of Drug Crizotinib

作　　者：弓添添 肖美娟 陈樱 何钰书 王普[1] GONG Tian-tian;XIAO Mei-juan;CHEN Ying;HE Yu-shu;WANG Pu(College of Pharmaceutical Science,Zhejiang University of Technology,Hangzhou,Zhejiang 310014,China)

机构地区：[1]浙江工业大学药学院,浙江杭州310014

出　　处：《浙江化工》2018年第10期10-14,共5页Zhejiang Chemical Industry

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

摘　　要：克唑替尼(Crizotinib)药物是全球第一个用于治疗非小细胞肺癌的可口服的分子靶向药物,也是治疗非小细胞肺癌晚期的首选药物。合成克唑替尼药物的难点和关键是其手性中间体(S)-1-(2,6-二氯-3-氟苯基)乙醇的制备。综述了克唑替尼关键手性中间体的合成方法,并对其制备技术的发展趋势进行了展望。Crizotinib is a kind of small molecule targeting drugs to cure non-small cell lung cancer （NSCLC）, which was also the preferred oral agents for NSCLC. How to obtain （S） - 1 - （2,6-dichloro-3-fluo- rophenyl）ethanol, a key intermediate of Crizotinib,is critical and hard in the preparation of Crizotinib. In this paper,the preparation technology of the key intermediate of Crizotinb is mainly introduced. The future devel- opment of Crizotinib preparation technology is also discussed.

关 键 词：克唑替尼 非小细胞肺癌 化学合成 生物催化 

分 类 号：R914[医药卫生—药物化学]