Synthetic Approaches to the New Drugs Approved During 2021

Abstract

Each year, new drugs are introduced to the market, representing structures that have affinity for biological targets implicated in human diseases and conditions. These new chemical entities (NCEs), particularly small molecules and antibody−drug conjugates, provide insight into molecular recognition and serve as potential leads for the design of future medicines. This annual review is part of a continuing series highlighting the most likely process-scale synthetic approaches to 35 NCEs that were first approved anywhere in the world during 2021. ■ SIGNIFICANCEThis publication presents a synopsis of the synthetic approaches to new drugs that were approved in 2021, based on the largest scale of synthesis that has been disclosed in primary literature and/or patents. This provides a view of the practical synthetic methods that are applicable to drug discovery and development and a holistic perspective on the molecular complexity of novel drug molecules and synthetic methods required to manufacture them.

Synthetic Approaches to the New Drugs Approved During 2022

“…The drugs highlighted in this review are organized into the following therapeutic areas: anti-infective and antibiotic, cardiovascular and hematologic, central nervous system, inflammation and immunologic, metabolic, oncology, and respiratory and pulmonary drug categories. This year’s review includes 23 drugs that were approved in 2022, as well as 11 drugs that were approved in 2021 or 2020 but were not covered in the previous years’ reviews. , The structures of the 34 drugs covered are shown in Figure .…”