Multicomponent reactions have been successfully applied as a platform for designing the step economical C–H activation-based organic synthesis wherein the in situ installation of directing group (DG) and the subsequent C–H activation-based amide arylation have been achieved in one-step. This multicomponent strategy allows the efficient synthesis of 2,6-biarylated or 6-arylated benzamides with significantly improved sustainability and discloses the potential of designing “ideal” synthesis by combining the concepts of C–H activation and multicomponent reaction.