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 fluoroalky...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.展开更多
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)。
文摘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.
