甾体激素6α位氟原子的引入方法  

The Method of Introducing 6α-Fluorine Atoms to Steroid

作　　者：张杰[1] 

机构地区：[1]天津天药药业股份有限公司,天津300462

出　　处：《辽宁化工》2017年第7期722-724,727,共4页Liaoning Chemical Industry

摘　　要：甾体激素上引入6α位氟原子可以明显增强其生理作用,甾体激素引入6α氟原子主要通过氟化试剂来实现,常用的氟化试剂有氟化氢、三氟化硼、过氯酰氟、氟化溴、NFPy、N-氟代磺酰亚胺等。通过比较各种氟化试剂的优缺点,我们认为新型的N-氟代磺酰亚胺、Selectfluor等为氟化试剂引入6α氟原子的方法较传统的氟化试剂相比,具有更高的立体选择性,毒性小,反应相对温和、安全。Introducing 6α-fluorine atoms to steroid can significantly enhance steroid＇s physiological function. In this article, various synthesis methods to 6-alpha fluorinated steroid were introduced. Advantages and disadvantages of different fluorinating agents were compared. The results show that new N-fluorosulfonimide and Selectfluor fluorinating agents are better than traditional fluorinating agents fluorination reagents because using these new fluorinating agents can obtain high stereoselectivity, and can make the reaction more moderate and safer.

关 键 词：甾体氟化 6α位氟化 氟化试剂 

分 类 号：TQ463[化学工程—制药化工]