The transition metal-mediated C–H bond activation has emerged as a powerful and ideal method for the total syntheses of natural products and pharmaceuticals, and has had a significant impact on synthetic planning and strategy in complex natural products.In this review, we describe selected recent examples of the transition metal-mediated C–H bond activation strategies for the rapid syntheses of natural products. The transition metal-mediated C-H bond activation has emerged as a powerful and ideal method for the total syntheses of natural products and pharmaceuticals, and has had a significant impact on synthetic planning and strategy in complex natural products. In this review, we describe selected recent examples of the transition metal-mediated C-H bond activation strategies for the rapid syntheses of natural products.