文献类型：期刊文献

英文题名：Tunable Synthesis of α-Amino Boronic Esters from Available Aldehydes and Amines through Sequential One-Pot Dehydration and Copper-Catalyzed Borylacylation

作者：Xia, Qi[1];Chang, Hua-Rong[1];Li, Juan[1];Wang, Jia-Yi[1];Peng, Yan-Qing[1];Song, Gong-Hua[1]

机构：[1]East China Univ Sci & Technol, Shanghai, Peoples R China

年份：2020

卷号：85

期号：4

起止页码：2716

外文期刊名：JOURNAL OF ORGANIC CHEMISTRY

收录：;EI(收录号：20200508096131);WOS:【SCI-EXPANDED(收录号:WOS:000516665800085)，CCR-EXPANDED(收录号:WOS:000516665800085)】；

基金：Financial support for this study from National Natural Science Foundation of China (Grant No. 21572060) and National Key Research and Development Plan (Grant No. 2017YFD0200504) is gratefully acknowledged.

语种：英文

外文关键词：Amines - Chlorine compounds - Catalysis - Copper

摘要：Copper-catalyzed multicomponent borylacylation of imines with acid chlorides and bis(pinacolato)diboron was developed for the preparation of synthetically useful and pharmacologically relevant alpha-amino boronic acid derivatives. Starting from a range of acid chlorides and imines with aryl, heteroaryl, and alkyl substituents, most of these ligand-free reactions proceeded smoothly at room temperature in moderate to good yields. Furthermore, a facile and convenient one-pot, multistep access to the direct synthesis of alpha-amino boronic acid derivatives from available aldehydes and amines was also developed.