A Four Azole Compounds Synthesis And Process Research

Nitrogen-containing heterocycles hold a special place among pharmaceutically important products with remarkable biological activities, which have been used widely in pharmaceutical and pesticide industry. So far, the synthesis of N-heterocycles has been studied as a hot chemical research area. Among these compounds, tetrazole is a kind of important five-membered heterocyclic compounds, which display anti-inflammatory, antimicrobial, and anti-allergic activities. Recent years, much attention has been paid to the studies of tetrazoles.The application and synthesis of tetrazoles using literature methods were summarized firstly. A proposed synthetic route for scale up was presented based on the analysis and comparison of different synthetic methods.Subsequently,5-bromo-N-tert-butyl-3-(1-phenyl-1//-tetrazol-5-yl)pyridin-2-amine was synthesized successfully. Different parameters including temperature, time, reagent, and solvent had been extensively investigated during the optimization process.The chemical structures of the products were identified with LCMS and NMR. The synthesis route is feasible, and the data obtained from optimization experiments would provide important support for the industrial production.