The realization of the direct CH bond functionalization has really brought the radical change in planning the organic synthetic strategies via traditional logics. The CH 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 CH bond functionalization of unactivated CH bonds of small organic scaffolds using different diazo carbonyl reagents, substrates, and catalysts‐controlled processes. This article has covered the selective and undirected CH 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 CH bond functionalization.