A kind of synthetic method of 1,5-substituted-1,2,3-triazole compounds

Abstract

The invention discloses a synthetic method of 1,5-substituted-1,2,3-triazole compounds and belongs to the technical field of triazole compounds. The technical scheme is characterized in that the synthetic method of the 1,5-substituted-1,2,3-triazole compounds adopts azide compounds and phosphorus ester compounds as substrates, tetramethyl guanidine as a catalyst and acetonitrile as a solvent, the components are stirred and subjected to a reaction at the temperature of 50-80 DEG C, and the 1,5-substituted-1,2,3-triazole compounds are prepared. The synthetic method has highly specific selectivity and can be used for effectively synthesizing the 1,5-substituted-1,2,3-triazole compounds containing different functional groups, reaction conditions are mild, and the usable range of the substrates is wide; a small organic molecule is utilized as the catalyst in the synthetic method, so that the usage of a metallic copper salt catalyst in a traditional click reaction is avoided, a product is effectively prevented from being polluted by trace metal ions, and the synthetic method has better application prospect in the field of pharmaceutical synthesis.

Description

technical field [0001] The invention belongs to the technical field of synthesis of triazole compounds, and in particular relates to a synthesis method of 1,5-substituted-1,2,3-triazole compounds. Background technique [0002] In recent years, molecules containing 1,2,3-triazoles have been widely used in the design and synthesis of bioactive molecules. As a class of important compounds with potential biological activity, 1,2,3-triazoles have a wide range of applications in the fields of organic synthesis, drug design, plant protection and materials. For example: HIV-1 protease inhibitors, anti-tumor inhibitors and non-nucleoside reverse transcriptase inhibitors all contain 1,2,3-triazole structure. At present, 1,5-disubstituted-1,2,3-triazole is already a very important pharmacophore and has a wide range of biological applications. However, expensive heavy metals, complex ligands and relatively harsh reaction conditions are commonly used in the method of synthesizing 1,5-s...

AI Technical Summary

Problems solved by technology

However, expensive heavy metals, complex ligands and relatively harsh reaction conditions are commonly used in the method of synthesizing 1,5-substituted-1,2,3-triazole compounds reported in the literature, and the existence of trace metal ions will affect the The application of the target product in the field of drug synthesis has a serious impact