Rapid assembly of α-ketoamides through a decarboxylative strategy of isocyanates with α-oxocarboxylic acids under mild conditions

作者：Huang, Junjie; Liang, Baihui; Chen, Xiuwen^*; Liu, Yifu; Li, Yawen; Liang, Jingwen; Zhu, Weidong; Tang, Xiaodong^*; Li, Yibiao; Zhu, Zhongzhi^*

来源：Organic and Biomolecular Chemistry, 2021, 19(21): 4783-4787.

DOI：10.1039/d1ob00562f

• CATALYZED DOUBLE CARBONYLATION
• METAL-FREE
• METHYL KETONES
• CHEMOSELECTIVE REDUCTION
• OXIDATIVE SYNTHESIS
• CARBON-MONOXIDE
• INHIBITORS
• AMINES
• AMIDES
• EFFICIENT

A simple and practical method for alpha-ketoamide synthesis via a decarboxylative strategy of isocyanates with alpha-oxocarboxylic acids is described. The reaction proceeds at room temperature under mild conditions without an oxidant or an additive, showing good substrate scope and functional compatibility. Moreover, the applicability of this method was further demonstrated by the synthesis of various bioactive molecules and different application examples through a two-step one-pot operation.

• 单位
  南方医科大学