Recent advances in the catalytic asymmetric construction of axially chiral azole-based frameworks

Abstract

Atropisomers featuring restricted rotation around a single bond have emerged as important structural motifs due to their prevalence in drug discovery, materials science and catalyst design. In recent years, the catalytic asymmetric synthesis of atropisomers has garnered significant fascination from chemists. While traditional six-membered axially chiral skeletons are commonly studied, methodologies directed towards less abundant five-membered heterobiaryls are relatively rare. In particular, axially chiral azole-based skeletons are essential components of five-membered heterocyclic frameworks and have received considerable interest. This review focuses on recent achievements in the atroposelective preparation of azole derivatives, by emphasizing mechanistic insights and synthetic applications. We hope that this review will encourage chemists worldwide to promote the continued development of this field in the future.