Synthetic Approaches to Piperazine-Containing Drugs Approved by FDA in the Period of 2011–2023
Maria Novella Romanelli,
Laura Braconi,
Alessio Gabellini,
Dina Manetti,
Giambattista Marotta,
Elisabetta Teodori
Affiliations
Maria Novella Romanelli
Section of Pharmaceutical and Nutraceutical Science, Department of Neurosciences, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Via Ugo Schiff, 6, Sesto Fiorentino, 50019 Florence, Italy
Laura Braconi
Section of Pharmaceutical and Nutraceutical Science, Department of Neurosciences, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Via Ugo Schiff, 6, Sesto Fiorentino, 50019 Florence, Italy
Alessio Gabellini
Section of Pharmaceutical and Nutraceutical Science, Department of Neurosciences, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Via Ugo Schiff, 6, Sesto Fiorentino, 50019 Florence, Italy
Dina Manetti
Section of Pharmaceutical and Nutraceutical Science, Department of Neurosciences, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Via Ugo Schiff, 6, Sesto Fiorentino, 50019 Florence, Italy
Giambattista Marotta
Section of Pharmaceutical and Nutraceutical Science, Department of Neurosciences, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Via Ugo Schiff, 6, Sesto Fiorentino, 50019 Florence, Italy
Elisabetta Teodori
Section of Pharmaceutical and Nutraceutical Science, Department of Neurosciences, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Via Ugo Schiff, 6, Sesto Fiorentino, 50019 Florence, Italy
The piperazine moiety is often found in drugs or in bioactive molecules. This widespread presence is due to different possible roles depending on the position in the molecule and on the therapeutic class, but it also depends on the chemical reactivity of piperazine-based synthons, which facilitate its insertion into the molecule. In this paper, we take into consideration the piperazine-containing drugs approved by the Food and Drug Administration between January 2011 and June 2023, and the synthetic methodologies used to prepare the compounds in the discovery and process chemistry are reviewed.
