Henan Key Laboratory of Organic Functional Molecules and Drug Innovation, Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, China.
J Org Chem. 2020 Nov 6;85(21):13710-13720. doi: 10.1021/acs.joc.0c01871. Epub 2020 Oct 28.
An efficient synthesis of α-amidoketone derivatives through the cascade reactions of carboxylic acids with vinyl azides is presented. Compared with literature protocols, notable features of this new method include catalyst-free conditions, broad substrate scope, good tolerance of a wide range of functional groups, and high efficiency. In addition, the synthetic potential of this method as a tool for late-stage modification was convincingly manifested by its application in the structural elaborations of a number of carboxylic acid drug molecules.
本文报道了一种通过羧酸与叠氮乙烯的级联反应高效合成α-酰胺酮衍生物的方法。与文献方法相比，该新方法具有显著特点，包括无催化剂条件、广泛的底物范围、对各种官能团的良好耐受性以及高效率。此外，该方法在一些羧酸药物分子的结构修饰中的应用充分证明了其作为后期修饰工具的合成潜力。
