Department of Biological & Synthetic Chemistry, Centre of Biomedical Research (CBMR), SGPGIMS Campus, Raebareli Road, Lucknow, 226014, Uttar Pradesh, India.
Angew Chem Int Ed Engl. 2023 Jan 9;62(2):e202210912. doi: 10.1002/anie.202210912. Epub 2022 Nov 28.
Over the past few years, the development of efficient methods to construct high-valued N-heterocyclic molecules have received massive attention owing to their extensive application in the areas of medicinal chemistry, drug discovery, natural product synthesis and so on. To access those high-valued N-heterocycles, many methods have been developed. In this context, transition-metal-catalyzed denitrogenative annulation of 1,2,3-triazoles and 1,2,3,4-tetrazoles has appeared as a powerful synthetic tool because it offers a step- and atom-economical route for the preparation of the nitrogen-rich molecules. Compared with the denitrogenative annulation of various 1,2,3-triazole frameworks, annulation of 1,2,3,4-tetrazole remains more challenging due to the inertness of the tetrazole moiety. This Review summarizes the significant achievements made in the field of denitrogenative annulation of various 1,2,3-triazoles and 1,2,3,4-tetrazoles including some pioneering examples in this area of research. We anticipate that this denitrogenative annulation reaction will find broad applications in the pharmaceutical industry, drug discovery and other fields of medicinal chemistry.
在过去的几年中，由于其在药物化学、药物发现、天然产物合成等领域的广泛应用，构建高价值 N-杂环分子的高效方法的发展受到了极大关注。为了获得这些高价值的 N-杂环化合物，已经开发了许多方法。在这种情况下，过渡金属催化的 1,2,3-三唑和 1,2,3,4-四唑的脱氮环化已成为一种强大的合成工具，因为它提供了一种步骤和原子经济性的方法来制备富氮分子。与各种 1,2,3-三唑骨架的脱氮环化相比，由于四唑部分的惰性，1,2,3,4-四唑的环化仍然更具挑战性。这篇综述总结了在各种 1,2,3-三唑和 1,2,3,4-四唑的脱氮环化领域所取得的重大成就，包括该研究领域的一些开创性实例。我们预计，这种脱氮环化反应将在制药工业、药物发现和药物化学的其他领域得到广泛应用。
