A practical access to fluoroalkylthio(seleno)-functionalized bicyclo[1.1.1]pentanes  

作　　者：Zhen Wu Yaohui Xu Jige Liu Xinxin Wu Chen Zhu 

机构地区：[1]Key Laboratory of Organic Synthesis of Jiangsu Province,College of Chemistry,Chemical Engineering and Materials Science,Soochow University,Suzhou 215125,China

出　　处：《Science China Chemistry》2020年第8期1025-1029,共5页中国科学（化学英文版）

基　　金：supported by the National Natural Science Foundation of China(21722205,21971173);the Project of Scientific and Technologic Infrastructure of Suzhou(SZS201905);the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)。

摘　　要：Rational design of new bioisosteres through introduction of high-value functional groups to bicyclo[1.1.1]pentane(BCP)is of particular use for drug discovery.Disclosed herein is the first access to valuable fluoroalkylthio(seleno)-functionalized BCPs.A range of SCF3,SCF2H,SCFH2,SeCF3,SeC4F9,and SeC8F17 groups are readily incorporated to BCPs under mild conditions.Concomitant installation of a sulfone provides a platform for incorporation of the BCP motif to bioactive molecules.This practical protocol features novel BCP scaffolds,broad substrate scope,excellent atom-economy,simple operation,and gramscale preparation.

关 键 词：bicyclo[1.1.1]pentane PROPELLANE bioisostere trifluoromethylthio trifluoromethylseleno 

分 类 号：TQ463[化学工程—制药化工]