Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Campus do Valonguinho, 24020-150, Niterói, RJ, Brazil.
Departamento de Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade Federal Fluminense, R. Dr. Mario Vianna, 523 - Santa Rosa, 24241-000, Niterói, RJ, Brazil.
Chem Rec. 2021 Oct;21(10):2782-2807. doi: 10.1002/tcr.202000185. Epub 2021 Feb 11.
The triazole heterocycle is a privileged scaffold in medicinal chemistry, since its structure is present in a large number of biologically active molecules, including several drugs currently in the market. Due to their vast applications, a wide variety of methods are described for their preparation, such as the 1,3-dipolar cycloaddition and processes involving diazo compounds and diazo transfer reactions. Considering the significant number of contributions from our research group to this chemistry in recent decades, in this account we discuss both the development of new methods for the synthesis of 1,2,3-triazoles and the preparation of new triazole-functionalized biologically active molecules using classical approaches.
三唑杂环是药物化学中的一个重要结构，因为它存在于大量具有生物活性的分子中，包括一些目前市场上的药物。由于其广泛的应用，已经有很多方法被用来制备三唑化合物，例如 1,3-偶极环加成和涉及重氮化合物和重氮转移反应的过程。考虑到我们研究小组在近几十年来对这一化学领域的大量贡献，在这篇综述中，我们讨论了新的 1,2,3-三唑合成方法的发展以及使用经典方法制备新的三唑功能化生物活性分子的进展。
