Synthetic Approaches to the New Drugs Approved During 2022

Abstract

In 2022, 23 new small molecule chemical entities were approved as drugs by the United States FDA, European Union EMA, Japan PMDA, and China NMPA. This review describes the synthetic approach demonstrated on largest scale for each new drug based on patent or primary literature. The synthetic routes highlight practical methods to construct molecules, sometimes on the manufacturing scale, to access the new drugs. Ten additional drugs approved in 2021 and one approved in 2020 are included that were not covered in the previous year's review. ■ SIGNFICANCEWith a brief discussion on the disease target and development background, this review focuses on synthetic routes to access new chemical entities including small molecules, antibody drug conjugates, and this year, a radioligand therapeutic. Drugs approved worldwide are included in the review.