Sustainable Synthesis of a Potent and Selective 5-HT₇ Receptor Antagonist Using a Mechanochemical Approach.

ABSTRACT: A mechanochemical procedure was developed to obtain PZ-1361, a potent and selective 5-HT₇ 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.

SUBMITTER: Canale V 

PROVIDER: S-EPMC7458427 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature