Sustainable Synthesis of a Potent and Selective 5-HT <sub>7</sub> Receptor Antagonist Using a Mechanochemical Approach
Vittorio Canale, Valeria Frisi, Xavier Bantreil, Frédéric Lamaty, Paweł Zajdel
Abstract
receptor antagonist, with antidepressant properties in rodents. The elaborated protocol offered several advantages over classical batch synthesis, including improvement of the overall yield (from 34% to 64%), reduction of reaction time (from 60 to 5.5 h), limitation of the use of toxic solvents, and the formation of byproducts. This approach represents a rare example of the synthesis of biologically active compounds exclusively performed using mechanochemical reactions.
Topics & Concepts
ChemistryAntagonistYield (engineering)Combinatorial chemistryChemical synthesisReceptor antagonistStereochemistryPharmacologyReceptorIn vitroBiochemistryMaterials scienceMedicineMetallurgyChemistry and Chemical EngineeringPhenothiazines and Benzothiazines Synthesis and ActivitiesComputational Drug Discovery Methods