In arene chemistry, CH direct functionalization has become one of the most attractive and challenge strategies for the introduction of new fragments bringing molecular complexity. Among a great number of transition metals involved in reaction approaches, Ru‐catalyzed CH functionalization of directed aryl‐containing compounds certainly provided unique reaction modes and new synthetic consideration in molecular design. In this article, we have overviewed the recent advances in the development of new synthetic approaches within the field of Ru‐catalyzed remote CH functionalization of directed arenes. The developments of the methodologies, synthetic applications, and reaction mechanisms on typical reaction modes have been discussed, and examples for accessing molecules in medicinal chemistry were also included.