Sustainable Synthesis of a Potent and Selective 5-HT7 Receptor Antagonist Using a Mechanochemical Approach.
J Org Chem
; 85(16): 10958-10965, 2020 08 21.
Article
in En
| MEDLINE
| ID: mdl-32706254
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Serotonin
/
Receptors, Serotonin
Language:
En
Journal:
J Org Chem
Year:
2020
Document type:
Article
Affiliation country:
Poland