文献类型：期刊文献

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

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

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Res Ctr Anal & Test, Sch Chem & Mol Engn, Shanghai 200237, Peoples R China

年份：2022

卷号：33

期号：11

起止页码：4817

外文期刊名：CHINESE CHEMICAL LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000851401100017)，CCR-EXPANDED(收录号:WOS:000851401100017)】；

基金：This work was financial supported by Innovation Program of Shanghai Municipal Education Commission (No. 201701070002E0 0 037). This work was also supported by National Key Research Program of China (No. 2017YFD0200505) and the Fundamental Research Funds for the Central Universities. We thank Prof. Youjun Yang for the help of revised the manuscript. The authors thank Research Center of Analysis and Test of East China University of Science and Technology for the characterization of the help on HRMS analysis.

语种：英文

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

摘要：Deuteriodifluoromethyl (CF2D) 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. (C) 2022 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.