Abstract In recent years, mechanochemistry has emerged as an innovative, viable, and eco‐friendly alternative to conventional solvent‐based synthesis, which enables rapid and selective construction of complex molecules. It has come to the forefront of organic synthesis owing to its greener aspects, such as elimination of bulk solvent, reduction in waste generation, shorter reaction times, ambient conditions, and better reaction yields. These advantages have rendered mechanochemistry highly desirable for industrial applications. This review provides a comprehensive summary of progress to date in the specific transformation with particular emphasis on metal‐catalyzed cross‐coupling reactions, oxidation and reduction reactions, C─H activation, and grindstone chemistry. We hope that this work will provide the researchers deeper insights into mechanochemical reactions and help them develop new synthetic strategies for advancing new frontiers in materials science and green chemistry.