应用化学2018，Vol.35Issue(5)：526-531,6.DOI:10.11944/j.issn.1000-0518.2018.05.170200
吡唑[1,5-a]并吡啶-3-羧酸衍生物合成方法的改进
Improved Synthesis of Pyrazolo[1,5-a] pyridine-3-carboxylic Acid Derivatives
摘要
Abstract
Pyrazolo[1,5-a] pyridine-3-carboxylate derivatives were obtained from 1,3-dipolar cycloaddition reaction with ethyl propionate and N-aminopyridine sulfates synthesized by the reactions of substituted pyridines and hydroxylamine-O-sulfonic acid.They were further treated with 30％NaOH aqueous solution to give corresponding substituted pyrazolo [ 1,5-a ] pyridine-3-carboxylic acid derivatives.In this method,N-aminopyridine sulfates were directly put into the next reaction,which eliminated the step of converting sulfate into iodine salt in the traditional method and solved the problem that the iodine salt was difficult to precipitate.N-aminopyridine sulfate and ethyl propionate were dissolved in water and N,N-dimethylformamide,respectively,and then mixed to increase the solubility of reactants.Six compounds(4a～4f)were successfully synthesized with yields of 88％～93％.The method is mild,easy to process and low cost as a new process for mass production.关键词
取代吡啶/羟胺-O-磺酸/偶极环加成/丙炔酸乙酯/吡唑[1,5-a]并吡啶-3-羧酸Key words
substituted pyridines/hydroxylamine-O-sulfonic acid/dipolar cycloaddition reaction/ethyl propionate/pyrazolo[1,5-a] pyridine-3-carboxylic acid分类
化学化工引用本文复制引用
徐娟,赵鑫雨,康从民..吡唑[1,5-a]并吡啶-3-羧酸衍生物合成方法的改进[J].应用化学,2018,35(5):526-531,6.基金项目
国家自然科学基金(21272131)资助 Supported by the National Natural Science Foundation of China(No.21272131) （21272131）
