Versatile Synthesis of Disubstituted Triazole Library for Dopamine and Serotonin Receptor Ligands†

Abstract

In the field of medicinal chemistry an extensive efforts have been made to explore potent and selective ligands for dopamine D3 1or D4 2 receptor for the discovery of antipsychotic drugs.3 Heterocyclic compounds bearing 1, 2, 3-triazole have long been the focus of synthetic chemistry due to their broad spectrum of applications in biological, pharmaceutical, and material areas.4,5 The incorporation of ‘click ’ chemistry,6,7 the Cu(I)-catalyzed Huisgen [2 + 3] dipolar cycloaddition reaction between an organic azide and an alkyne to form 1,4-disubstituted tirazoles with exclusive selectivity, has recently become a laboratorial preference toward the construction of compound libraries,8 along with applications in organic chemistry,9,10 drug discovery.1