Catalytic macrocyclization of unactivated C(sp3)-H bond in natural product synthesis

Abstract

Macrocyclic natural products present as essential scaffolds in drug development. Excited by the biological properties of macrocyclic natural products, its synthesis and the development of macrocyclization methods is an important research area in organic and medicinal chemistry. In particular, macrocyclization preparing macrocyclic structures via catalytic functionalization of unactivated C(sp³)-H bonds is increasingly prevalent in the literature. Here, we provide a minireview highlighting the contemporary advancements of catalytic macrocyclization of unactivated C(sp³)-H bond in method developments and natural product synthesis. Representative examples from 2017 to 2024 are discussed.