Selective functionalization of benzylic C(sp3)-H bonds to synthesize complex molecules

Functionalization of the benzylic C(sp(3))-H bond has become a compelling and robust tool to speed up pre-clinical research for lead discovery. Besides bring frequently utilizated to construct complex molecules in total synthesis, this emerging strategy of benzylic C(sp(3))-H bond functionalization has facilitated site-selective modifications of complex molecules. Here, we have summarized recent benzylic C(sp(3))-H bond functionalization applications for synthesizing complex molecules. We have carefully addressed recent applications in this topic, ranging from the site-selective modifications using benzylic C-H bond functionalization to the total synthesis of natural products. This review will recount the formation and application of new C-C, C-O, C-N, and C-X (X = halogens, sulfur, etc.) bonds to provide a clear blueprint for and deep insight into the functionalization of benzylic C-H bonds.

Automated summary

The functionalization of the benzylic C(sp(3))-H bond is a powerful tool in pre-clinical research for lead discovery. It enables site-selective modifications and total synthesis of complex molecules, providing valuable insights into the formation and application of new C-C, C-O, C-N, and C-X bonds.