Abstract Transition metal catalyzed C─H activation is a dynamic synthetic route for coupling reactions in the field of chemistry, which has been developed over the last 20 years. The C─H activation approach for achieving C─C bond cross‐coupling reactions avoids all elements of pre‐functionalized substrates and lengthy synthetic routes. Pyridine‐derived moieties are indispensable in directed C─H bond activation by selective direction of the transition metal catalyst to bind C─H bonds in the phenyl ring. This review focuses on the rhodium(III)‐catalyzed direct functionalization of C─H bonds under oxidative conditions, enabling the formation of C─C, C─N, and C─O bonds of 2‐phenylpyridines to functionalized products with an emphasis on reports from 2009. The efficient creation of C─E bonds (where E═C, N, S, or O) makes Rh(III) catalysis an appealing, step‐efficient method for producing value‐added molecules from readily available starting materials. Focus is given to the significant regioselectivity and functional group tolerance of each reaction mechanism, along with a brief discussion of a few mechanistic pathways. Also demonstrates considerable scientific progress and greater advances, particularly in developing functionalized systems via transition metal‐catalyzed C─H activation with practical applications in the pharmaceutical industries, agrochemical industry, and drug discovery.