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Article Dans Une Revue Journal of Organic Chemistry Année : 2020

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

Résumé

A mechanochemical procedure was developed to obtain PZ-1361, a potent and selective 5-HT 7 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 .
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Dates et versions

hal-02925108 , version 1 (01-09-2020)

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Vittorio Canale, Valeria Frisi, Xavier Bantreil, Frédéric Lamaty, Paweł Zajdel. Sustainable Synthesis of a Potent and Selective 5-HT7 Receptor Antagonist Using a Mechanochemical Approach. Journal of Organic Chemistry, 2020, 85 (16), pp.10958-10965. ⟨10.1021/acs.joc.0c01044⟩. ⟨hal-02925108⟩
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