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.
Keywords: Asymmetric synthesis, Bio-active molecules, Piperazine, Rearrangement reaction, Synthetic strategies.
