3-取代-6,7-二氢-5H-吡咯[2,1-c][1,2,4]三唑-5-羧酸甲酯的合成研究  

Synthesis of 3-Substituent-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole-5-carboxylic Acid Methyl Ester

作　　者：曹国锐[1] 王赛[1] 吴燕天 滕大为[1] 

机构地区：[1]青岛科技大学化工学院,山东青岛266042

出　　处：《化学试剂》2016年第5期475-480,共6页Chemical Reagents

基　　金：山东省自然科学基金资助项目(ZR2014BL028)

摘　　要：以2．吡咯烷酮-5-羧酸甲酯为原料，经甲基化、取代和环合等反应，合成了16个目标化合物，其中13个为新化合物，其结构经。HNMR和HR-MS确证。并且研究了环合反应条件，确定了环合反应的溶剂、催化剂及用量，即以氯苯为溶剂，2mol％的醋酸为催化剂。该合成方法环合条件温和、操作简单，具有较强的通用性。Sixteen 3-substituted-6,7-dihydro-5 H-pyrrolo [ 2,1 -c ] [ 1,2,4 ] triazole-5-carboxylic acid methyl ester were synthesized by the reaction of methylation, substitution and cyclization from 5-oxo-pyrrolidine-2-carboxylic acid methyl ester. The structures were confirmed by I HNMR and HR-MS. A series of solvent,catalyst and amount of catalyst were evaluated and 2 mol% of acetic acid was identified as the best catalyst for the cyclization with chlorobenzene as solvent. The method is easy to operate under mild reaction condition and can be wildly used.

关 键 词：2-吡咯烷酮-5-羧酸甲酯 合成 吡咯[2 1-c][1 2 4]三唑-5-羧酸甲酯 环合反应 

分 类 号：O626[理学—有机化学]