Asymmetric Synthesis of Biologically Active Piperazine Derivatives

An emerging area of interest in medicinal chemistry has highlighted heterocyclic moieties as some of the most promising compounds in organic chemistry. Piperazine is a notable six-membered saturated N-heterocyclic moiety with a wide range of bioactive applications in the pharmaceutical industry. Molecules containing the piperazine core unit have demonstrated numerous beneficial activities, such as antibacterial, analgesic, antiviral, antihypertensive, anti-allergic, antimalarial, antipsychotic, antidepressant, cardioprotective, antifungal, antioxidant, antiinflammatory, and anticancer properties. The Food and Drug Administration (FDA) has approved various piperazine-based drugs for the treatment of several viral diseases, underscoring the pharmacological significance of piperazine analogues. In this chapter, we discuss in detail the procedures for the asymmetric synthesis of biologically active piperazine and its derivatives.