Abstract

Abstract The realization of the direct CH bond functionalization has really brought the radical change in planning the organic synthetic strategies via traditional logics. The CH bond functionalization is an art of selective functionalization even in presence of more reactive functional groups. In this article, we have highlighted more challenging intermolecular site‐selective CH bond functionalization of unactivated CH bonds of small organic scaffolds using different diazo carbonyl reagents, substrates, and catalysts‐controlled processes. This article has covered the selective and undirected CH functionalization of alkanes, arenes, N ‐substituted and free aromatic amines, phenols, naphthols, 1,3‐dicarbonyl compounds, and benzofurans with different diazo carbonyl compounds under metal catalysis. This article has been written to serve as a guide for understanding the principle and for accessing newer approaches to achieve the selective CH bond functionalization.

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