文献类型：期刊文献

中文题名：A bench-stable reagent for C-4 selective deuteriodifluoromethylation of azines

作者：Junqing Liang[1];Lefeng Dong[1];Feng Qian[2];Yijin Kong[1];Mingxia Wang[1];Xiaoyong Xu[1];Xusheng Shao[1];Zhong Li[1]

机构：[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

年份：2022

卷号：33

期号：11

起止页码：4817

中文期刊名：Chinese Chemical Letters

外文期刊名：中国化学快报（英文版）

收录：CSTPCD;;Scopus;CSCD:【CSCD2021_2022】；PubMed;

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。

语种：英文

中文关键词：Reagent;Deuterium;Difluoromethylation;C-4 selective;Azines

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.