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

preprint
submitted on 15.04.2020 and posted on 17.04.2020 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.

Funding

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

History

Email Address of Submitting Author

vittorio.canale@uj.edu.pl

Institution

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

Country

Poland

ORCID For Submitting Author

0000-0001-7940-9500

Declaration of Conflict of Interest

There are no conflicts of interest to declare

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