A bench-stable reagent for C-4 selective deuteriodifluoromethylation of azines  

作　　者：Junqing Liang Lefeng Dong Feng Qian Yijin Kong Mingxia Wang Xiaoyong Xu Xusheng Shao Zhong Li 

机构地区：[1]Shanghai Key Laboratory of Chemical Biology,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China [2]Research Center of Analysis and Test,School of Chemistry and Molecular Engineering,East China University of Science and Technology,Shanghai 200237,China

出　　处：《Chinese Chemical Letters》2022年第11期4817-4821,共5页中国化学快报（英文版）

基　　金：financial supported by Innovation Program of Shanghai Municipal Education Commission(No.201701070002E00037);supported by National Key Research Program of China(No.2017YFD0200505);the Fundamental Research Funds for the Central Universities。

摘　　要：Deuteriodifluoromethyl(CF_(2)D)is a challenging and important functional group due to difficult deuterium incorporation and lack of effective precursor reagents.Herein,we report a bench-stable reagent,deuteriodifluoromethyl phosphine(DDFP)from cheap deuterium source for selectivity deuteriodifluoromethylation of azines with a high deuterium incorporation yield.The late-stage modification of complex molecules further confirmed the potential of this reagent for practical applications.We expect that our reagent to find applications in synthesis of isotope-labelled molecules of interests for drug-discovery and related ilucidation of mechanism of action.

关 键 词：REAGENT DEUTERIUM DIFLUOROMETHYLATION C-4 selective AZINES 

分 类 号：TQ460.1[化学工程—制药化工]