Abstract

The useful physiological activity of pharmaceuticals containing asymmetric center(s) appears usually in only one enantiomer. Hence, an effective synthesis of the desired enantiomer with optical purity is now an important subject in chemistry. The chiral synthon has been obtained by asymmetric chemical synthesis, synthesis of a racemate followed by its optical resolution, chiral induction in a specific prochiral compound with enzymes or micro-organisms, and chemical transformation from easily available sugars, amino acids, terpenoids, and other optically active natural products. An overview of chiral designs, reactions, and applications are discussed in this chapter. Novel chiral designs using functional and chiral heterocycles seem likely in the future, especially when used in combination with organometallic reagents and/or molecular symmetry. Creative investigations employing such chiral heterocycles and related compounds will be extensively pursued.

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