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

Department of Chemistry, Rutgers University, 73 Warren Street, Newark, NJ 07102, USA
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Author to whom correspondence should be addressed.
Academic Editor: Stéphane P. Roche
Received: 25 August 2021 / Revised: 7 September 2021 / Accepted: 16 September 2021 / Published: 8 October 2021
(This article belongs to the Special Issue Feature Papers in Organics)
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. View Full-Text
Keywords: piperazines; N-heterocycles; C–H functionalization; photoredox; heterocyclic chemistry; six-membered heterocycles; nitrogen heterocycles; drug discovery; medicinal chemistry piperazines; N-heterocycles; C–H functionalization; photoredox; heterocyclic chemistry; six-membered heterocycles; nitrogen heterocycles; drug discovery; medicinal chemistry
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MDPI and ACS Style

Durand, C.; Szostak, M. Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization. Organics 2021, 2, 337-347. https://0-doi-org.brum.beds.ac.uk/10.3390/org2040018

AMA Style

Durand C, Szostak M. Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization. Organics. 2021; 2(4):337-347. https://0-doi-org.brum.beds.ac.uk/10.3390/org2040018

Chicago/Turabian Style

Durand, Carolina, and Michal Szostak. 2021. "Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization" Organics 2, no. 4: 337-347. https://0-doi-org.brum.beds.ac.uk/10.3390/org2040018

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