α-C(sp³)-H arylation is an important type of C-H functionalization. Various biologically significant natural products, chemical intermediates, and drugs have been effectively prepared via C-H functionalization. Cyclic carbonyl compounds comprise of cyclic ketones, enones, lactones, and lactams. The α-C(sp³)-H arylation of these compounds have been exhibited high efficiency in forming C(sp³)-C(sp²) bonds, played a crucial role in organic synthesis, and attracted majority of interests from organic and medicinal communities. This review focused on the most significant advances including methods, mechanism, and applications in total synthesis of natural products in the field of α-C(sp³)-H arylations of cyclic carbonyl compounds in recent years.

α -C(sp ³ )-H芳基化是CH官能化的一种重要类型。通过CH官能化可以有效地制备各种具有生物学意义的天然产物、化学中间体和药物。环状羰基化合物包括环状酮、烯酮、内酯和内酰胺。这些化合物的α - C(sp ^{3 )-H芳基化在形成C(sp 3} )-C(sp ² )键方面表现出高效，在有机合成中发挥着至关重要的作用，并引起了有机和化学界的广泛关注。医药社区。本文重点综述了近年来环状羰基化合物α -C(sp ³ )-H芳基化领域在天然产物全合成中的方法、机理和应用等最重要的进展。