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在温和条件下,通过异氰酸酯与α-氧代羧酸的脱羧策略快速组装α-酮酰胺。

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

机构信息

School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, China.

Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.

出版信息

Org Biomol Chem. 2021 Jun 2;19(21):4783-4787. doi: 10.1039/d1ob00562f.

Abstract

A simple and practical method for α-ketoamide synthesis via a decarboxylative strategy of isocyanates with α-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.

摘要

本文描述了一种通过异氰酸酯与α-氧代羧酸的脱羧策略合成α-酮酰胺的简单实用方法。该反应在温和条件下于室温下进行,无需氧化剂或添加剂,具有良好的底物范围和功能相容性。此外,通过两步一锅操作,进一步通过合成各种生物活性分子和不同应用实例证明了该方法的适用性。

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