General Approach to Amides through Decarboxylative Radical Cross-Coupling of Carboxylic Acids and Isocyanides

Herein, we report a silver-catalyzed protocol for decarboxylative cross-coupling between carboxylic acids and isocyanides, leading to linear amide products through a free-radical mechanism. The disclosed approach provides a general entry to a variety of decorated amides, accommodating a diverse array of radical precursors, including aryl, heteroaryl, alkynyl, alkenyl, and alkyl carboxylic acids. Notably, the protocol proved to be efficient for decarboxylative late-stage functionalization of several elaborate pharmaceuticals, demonstrating its potential applications.

本文报道了一种银催化的羧酸与异氰化物之间的脱羧交叉偶联反应策略，该策略通过自由基机理生成直链酰胺产物。本公开方法可为多种取代酰胺的合成提供通用途径，可兼容包括芳基、杂芳基、炔基、烯基以及烷基羧酸在内的各类自由基前体。值得注意的是，该策略对多种复杂药物分子的脱羧后期官能化展现出高效的反应性能，证实了其潜在应用价值。