Copper-Catalyzed Oxalamide-Directed <i>ortho</i>-C–H Amination of Anilines with Alkylamines
作者:Peng Wu、Wei Huang、Tai-Jin Cheng、Hai-Xia Lin、Hui Xu、Hui-Xiong Dai
DOI:10.1021/acs.orglett.0c01632
日期:2020.7.2
A copper-catalyzed oxalamide-directed ortho-C-H amination of anilines has been developed by using 1 atm of air as the sole oxidant. The protocol shows excellent functional group tolerance, and some heterocyclic amines including indole, benzothiophene, benzothiazole, quinoline, isoquinoline, and quinoxaline could be compatible in the reaction. The late-stage diversification of medicinal drugs demonstrates the synthetic utility of this protocol.
Hydrogen peroxide-promoted metal free oxidative amidation of 2-oxoaldehydes: a facile access to unsymmetrical oxamides
A novel and green H2O2-promoted oxidative amidation of 2-oxoaldehydes with amines to synthesize unsymmetrical oxamides has been developed. The reactions proceeded smoothly at room temperature under metal-free conditions and generated the corresponding products in good yields. This methodology has a broad substrate scope and opens up an interesting and attractive avenue for the synthesis of unsymmetrical
已开发出新颖且绿色的H 2 O 2促进的2-氧代醛与胺的氧化酰胺化反应,以合成不对称的草酰胺。反应在室温下在无金属的条件下平稳进行,并以良好的产率产生相应的产物。该方法具有广泛的底物范围,并为合成不对称的草酰胺衍生物开辟了有趣的诱人途径。