Difluoroalkylative carbonylation of alkenes to access carbonyl difluoro-containing heterocycles:convenient synthesis of gemigliptin

作     者：Zhi-Peng Bao Youcan Zhang Le-Cheng Wang Xiao-Feng Wu 

作者机构：Dalian National Laboratory for Clean EnergyDalian Institute of Chemical PhysicsChinese Academy of SciencesDalian 116023China Leibniz-Institut für Katalyse e.V.Albert-Einstein-Straße 29aRostock 18059Germany 

出 版 物：《Science China Chemistry》 (中国科学（化学英文版）)

年 卷 期：2023年第66卷第1期

页      面：139-146页

核心收录：

学科分类：07[理学] 0828[工学-农业工程] 0903[农学-农业资源与环境] 070303[理学-有机化学] 0703[理学-化学] 

基　　金：supported by the DICP and K.C.Wong Education Foundation(GJTD-2020-08)。 

主　　题：difluoroalkylative carbonylative unactivated alkenes ethylene gas heterocycles 

摘      要：Fluorinated heterocycles play a vital role in pharmaceutical and agrochemical industries.Hence,rapid and efficient construction of fluorinated heterocycles remains highly demanded.Herein,a difluoroalkylative carbonylative cyclization of unactivated alkenes and ethylene gas enabled by palladium catalysis has been developed for the first time toward the synthesis ofα-carbonyl difluoro-modified glutarimides.This procedure can also be applied to the synthesis of Ge Migliptin which is a medicine approved for the treatment of type 2 diabetes mellitus.