Recent Advances in the Asymmetric Total Synthesis of Camptothecin

During the past decades, a variety of routes for the total synthesis of camptothecin have been reported. Considering only (S)-camptothecin and (S)-camptothecin analogues possessing the ability to inhibit DNA enzyme topoisomerase I, numerous advances have been achieved for the asymmetric total synthesis of camptothecin, providing concise and scalable approaches to (S)-camptothecin for the academic community and pharmaceutical industry. This review outlines recent advances in the asymmetric total synthesis of camptothecin, and is timely and highly desirable for the rapid development of this field. By constructing the chiral tertiary alcohol center, diverse attractive strategies have been developed for the total synthesis of (S)-camptothecin. © 2022 Wiley-VCH GmbH.