Abstract Selective carbon–carbon bond‐formation reactions are described via gold‐catalyzed CH bond activation. Gold catalysis has indeed emerged as an extraordinary tool for the scientific community. We disclose in this article selected and seminal examples implying the functionalization of alkynes, the C(sp 2 )H bonds, and the C(sp 3 )H bonds. In each section, the asymmetric versions and applications in the total synthesis are invoked, and we highlight the most recent examples described in the bibliography.