Mild and Metal‐Free Cross‐Dehydrogenative Coupling of Nitrogen Heteroarenes with Aldehydes Enabled by Structural Hybridization of Promoting Reagents

Abstract

A mild and metal-free cross-dehydrogenative coupling reaction of nitrogen heteroarenes with aldehydes has been developed by the structural hybridization of promoting reagents. The procedure is environmentally benign, cost-effective and industrially scalable, which allows the direct acylation of electron-deficient nitrogen heteroarenes in moderate to good yields. Furthermore, the synthetic utility of this new method in the synthesis of a variety of pharmaceutically relevant isoquinoline alkaloids has been also demonstrated. conditions using iron sulfate as an alternative promoter, while low reaction efficiency and rather limited substrate scope are typically observed (Scheme 1b). [5] Recently, a visible lightmediated CDC at room temperature was introduced by Lei [a] Dr.