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Updated: Oct 3, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT(3) ligands
Isabel Iriepa1, Francisco J Villasante, Enrique Gálvez
1Departamento de Química Orgánica, Universidad de Alcalá, Ctra. Madrid-Barcelona Km. 33,600, 28871 Alcalá de Henares, Madrid, Spain. isabel.iriepa@uah.es
Abstract:
A series of 4-amino-5-chloro-2-methoxybenzoates and benzamides containing the 5- and 6-isoquinuclidinyl system was synthesised and evaluated for binding to 5-HT(3), 5-HT(4) and D(2) receptors. In general, the isoquinuclidine derivatives at the 5-position have shown to be more potent as 5-HT(3) ligands but they also possess 5-HT(4) and D(2) properties. However, the results show that the derivatives at the 6-position afforded the most promising compounds in terms of both receptor affinity and selectivity.
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