铜催化的酰亚胺导向的苯胺与脂肪胺的 -C-H 胺化反应。
Copper-Catalyzed Oxalamide-Directed -C-H Amination of Anilines with Alkylamines.
机构信息
Department of Chemistry, Innovative Drug Research Center, Shanghai University, 99 Shangda Road, Shanghai 200444, China.
School of Pharmacy, Nanchang University, 461 Bayi Road, Nanchang 330006, China.
出版信息
Org Lett. 2020 Jul 2;22(13):5051-5056. doi: 10.1021/acs.orglett.0c01632. Epub 2020 Jun 16.
A copper-catalyzed oxalamide-directed -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.
发展了一种铜催化的、以草酰二胺为导向的苯胺 -C-H 氨化反应，该反应仅使用 1 个大气压的空气作为唯一氧化剂。该反应条件具有很好的官能团容忍性，一些杂环胺，包括吲哚、苯并噻吩、苯并噻唑、喹啉、异喹啉和喹喔啉，都能兼容于该反应体系。该方法还可用于药物的后期多样化合成，进一步证明了该方法具有合成实用性。
Zotero 插件