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Transition metal catalyzed C–H activation has surfaced as a powerful tool to improve the efficacy of molecular synthesis. Last two decades have witnessed a considerable progress in the activation of otherwise inert C–H bonds. However, during recent years, focus has shifted to address rising concerns to achieve high levels of resource economy in molecular syntheses. Herein, we discuss the advent and recent emerging strategies to improve the sustainability and environmentally benign nature of C–H activation manifolds.