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

submitted on 15.04.2020, 11:59 and posted on 17.04.2020, 08:26 by Vittorio Canale, Valeria Frisi, Xavier Bantreil, Frédéric Lamaty, Paweł Zajdel

Recently, ball milling has become an excellent tool in synthetic organic chemistry as it offers several advantages over classical batch synthesis. Here, an efficient and sustainable mechanochemical procedure was developed to obtain PZ-1361, a potent and selective 5-HT7 receptor antagonist, with significant antidepressant properties in rodents. The elaborated protocol limited the use of organic solvents, reduced the excess of the alkylating agent, and enabled to avoid column chromatography purification of intermediates and the final compound.


statutory grant of Jagiellonian University Medical College no N42/DBS/000018,

National Science Center, Poland no grant 2019/33/B/NZ7/02822

PHC Polonium program


Email Address of Submitting Author


Jagiellonian University Medical College, Faculty of Pharmacy, Department of Medicinal Chemistry



ORCID For Submitting Author


Declaration of Conflict of Interest

There are no conflicts of interest to declare