Dynamic Axial Chirality in Drug Design and Discovery: Introduction to Atropisomerism, Classification, Significance, Recent Trends and Challenges

Abstract

Induction of chirality in non-chiral ligands via involvement of hindered rotation around a single bond has led to the development of atropisomers. The atropisomers behave similarly as the chiral compounds and impact the drug discovery process. The chapter deals importantly with the brief introduction to this class, nomenclature descriptors, methods to measure atropisomers racemization, and the impact of atropisomers on drug discovery and includes relevant examples of drugs both from synthetic and natural origin. The chapter further extends to deal with various methodologies involved in atropselective conversions and regulatory guidelines involved in the development of atropisomers. � Springer Nature Singapore Pte Ltd. 2021.