Enantioselective Transformations in the Synthesis of Therapeutic Agents

Theproportion of approved chiral drugs and drug candidatesundermedical studies has surged dramatically over the past two decades.As a consequence, the efficient synthesis of enantiopure pharmaceuticalsor their synthetic intermediates poses a profound challenge to medicinaland process chemists. The significant advancement in asymmetric catalysishas provided an effective and reliable solution to this challenge.The successful application of transition metal catalysis, organocatalysis,and biocatalysis to the medicinal and pharmaceutical industries haspromoted drug discovery by efficient and precise preparation of enantio-enrichedtherapeutic agents, and facilitated the industrial production of activepharmaceutical ingredient in an economic and environmentally friendlyfashion. The present review summarizes the most recent applications(2008-2022) of asymmetric catalysis in the pharmaceutical industryranging from process scales to pilot and industrial levels. It alsoshowcases the latest achievements and trends in the asymmetric synthesisof therapeutic agents with state of the art technologies of asymmetriccatalysis.

Automated summary

In the past two decades, there has been a significant increase in the proportion of approved chiral drugs and drug candidates under medical studies. This has posed a challenge for medicinal and process chemists in efficiently synthesizing enantiopure pharmaceuticals. However, the development of asymmetric catalysis has provided an effective solution to this challenge, promoting drug discovery and industrial production of active pharmaceutical ingredients in an economic and environmentally friendly manner. This review summarizes the recent applications of asymmetric catalysis in the pharmaceutical industry, showcasing the achievements and trends in the asymmetric synthesis of therapeutic agents using state-of-the-art technologies.