CCNU-uOttawa Joint Research Centre, Key Laboratory of Pesticides & Chemical Biology Ministry of Education, Interna-tional Joint Research Center for Intelligent Biosensing Technology and Health, College of Chemistry, Central China Normal University, 152 Luoyu Road, Wuhan, Hubei 430079, China.
Chem Commun (Camb). 2021 May 11;57(38):4674-4677. doi: 10.1039/d1cc00663k.
The highly enantioselective copper-catalyzed propargylic amination of propargylic esters with amine hydrochloride salts has been realized for the first time using copper salts with chiral N,N,P-ligands. This method features a broad substrate scope and wide functional group tolerance, generating propargylic amines in good to excellent yields with high enantioselectivities (up to 99% ee). The utility of the approach was demonstrated by late-stage functionalization of marketed pharmaceuticals.
首次使用手性 N,N,P-配体的铜盐实现了对炔丙基酯与胺盐酸盐的高对映选择性铜催化炔丙基胺化反应。该方法具有广泛的底物范围和广泛的官能团容忍性，能够以良好到优秀的收率和高对映选择性（高达 99%ee）生成炔丙基胺。该方法的实用性通过对市售药物的后期官能化得到了证明。
