甾体激素引入6α氟原子的各种方法  

Introduction Methods of 6α-Fluoro to Steroid Hormone

作　　者：郭罕奇[1] 裴文[1] 

机构地区：[1]浙江工业大学化学工程与材料学院,杭州310014

出　　处：《化工生产与技术》2010年第3期1-3,13,共4页Chemical Production and Technology

摘　　要：叙述了利用氟化氢、三氟化硼、过氯酰氟、2-氯-1,1,2-三氟三乙胺氟化溴、亲电试剂NFPy和N-氟代磺酰亚胺氟化剂向甾体激素引入6α氟原子的方法,比较了各种方法的优缺点,认为N-氟代磺酰亚胺为氟化试剂引入6α氟原子的方法N-氟代磺酰亚胺氟化试剂,具有高立体选择性,毒性小,反应相对温和、安全。Introduction methods of 6α-fluoro atoms to steroid hormone with hydrogen fluoride,boron trifluoride and perchloryl fluoride,2-chloro-1,1,2-trifluorotriethylamine,bromine fluoride,electrophilic reagent NFPy and n-fluorosulphonylimide fluorinating agent are described.Advantages and disadvantages of all kinds of methods are compared.It is regarded in the method of 6α-fluoro atoms to steroid hormone with n-fluorosulphonylimide fluorinating agent,as n-fluorosulphonylimide fluorinating agent is highly stereoselective with little toxicity,the reaction is relatively mild and safe.

关 键 词：甾体激素 氟化 N-氟代磺酰亚胺合成 

分 类 号：TQ467.8[化学工程—制药化工]