The chapter gives an insight into the chemistry of chiral pharmaceuticals,
discussing the different classes of compounds that have been synthesized using
asymmetric methods. It covers the synthetic routes used to produce chiral
pharmaceuticals and discusses the impact of chirality on their pharmacological
properties. The chapter discusses key challenges in developing enantioselective
syntheses for complex drug molecules, particularly those with intricate structures and
multiple stereo-enters. It examines issues like controlling stereoselectivity, optimizing
reaction conditions, and scaling up for industrial use. Additionally, the chapter explores
the biological activities of chiral heterocycles, emphasizing how their stereochemistry
impacts drug potency, selectivity, and metabolism. It highlights both the importance of
enantioselective synthesis and the critical role of chiral heterocycles in the
effectiveness of modern pharmaceuticals.
Keywords: Asymmetric synthesis, Biological activities, Chiral compounds, Chiral pharmaceuticals.