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Research Article Open access CC BY 4.0

Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization

Carolina Durand, Michal Szostak

Organics · pp. 337–347 · Published 8 Oct 2021

10.3390/org2040018

Abstract

Piperazine ranks as the third most common nitrogen heterocycle in drug discovery, and it is the key component of several blockbuster drugs, such as Imatinib (also marketed as Gleevec) or Sildenafil, sold as Viagra. Despite its wide use in medicinal chemistry, the structural diversity of piperazines is limited, with about 80% of piperazine-containing drugs containing substituents only at the nitrogen positions. Recently, major advances have been made in the C–H functionalization of the carbon atoms of the piperazine ring. Herein, we present an overview of the recent synthetic methods to afford functionalized piperazines with a focus on C–H functionalization.

Piperazine Surface modification Chemistry Ring (chemistry) Combinatorial chemistry Organic chemistry Physical chemistry

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