Copper chemistry has great importance owing to its low cost, high functional group tolerance, high abundance, and low toxicity. In addition to natural copper-containing catalysts, significant efforts have been devoted toward the development of man-made copper redox catalysts. Apart from these efforts, copper has become one of the most versatile and interesting bio-relevant metals in homogeneous catalysis. The chapter also provides an overview of the key concepts discussed in this book. The book concentrates on various copper-catalyzed organic transformations covering areas such as heterocyclic synthesis, coupling reactions, asymmetric synthesis, click reactions, multicomponent reactions, C–H activation, trifluoromethylation reactions, and applications in the synthesis of natural products. Copper-catalyzed heterocyclic synthesis and multicomponent reactions were found to be important tools toward the synthesis of many biologically active compounds. The book summarizes the developments in copper catalysis in the field of organic chemistry and discusses the future perspectives of copper catalysis for contemporary organic synthesis.