C-H bonds are ubiquitous in organic molecules. Homogenous gold-catalyzed direct functionalization of unsaturated C-H bonds has emerged as a powerful method in our synthetic toolbox. However, Csp(3)-H bonds have larger dissociation energy and lower proton acidity, and thus the efficient and exquisitely selective cleavage of this kind of chemical bonds for the formation of new carbon-carbon and carbon-heteroatom bonds is still a great challenge. In this tutorial review, we will highlight the recent achievements of gold-catalyzed oxidative and redox-neutral Csp(3)-H bond functionalization, which opens new avenues for economical and sustainable construction of fine chemicals.