一步法合成1,2,4-三氮唑[3,4-i]嘌呤类化合物  

One-Step Synthesis of 1,2,4-Triazolo[3,4-i]purine Derivatives

作　　者：楚治良 陈晖娟 单帅 王晓娜[1] 高春芳[1] 渠桂荣[2] 刘忠于 郭海明[2] Chu Zhiliang;Chen Huijuan;Shan Shuai;Wang Xiaona;Gao Chunfang;Qu Guirong;Liu Zhongyu;Guo Haiming(The 989th Hospital of the Joint Logistics Support Force of Chinese People's Liberation Army,Luoyang,Henan 471031;School of Chemistry and Chemical Engineering,Henan Normal University,Xinxiang,Henan 453007)

机构地区：[1]中国人民解放军联勤保障部队第989医院,河南洛阳471031 [2]河南师范大学化学化工学院,河南新乡453007

出　　处：《有机化学》2022年第5期1551-1556,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.U1604283);国家科技重大专项(No.2014ZX09J14101-01A);洛阳市科技计划医疗卫生(No.1720001A-8)资助项目。

摘　　要：1,2,4-三氮唑[3,4-i]嘌呤类化合物是潜在的黄嘌呤氧化酶(XO)抑制剂,有望用于痛风的治疗.报道了一种一步合成1,2,4-三氮唑[3,4-i]嘌呤类化合物的新方法.以6-肼基-N^(9)-取代嘌呤和脂肪族一元羧酸为原料,无水硫酸镁作除水剂,合成了17个新化合物.该方法操作简单,无需使用其他催化剂和氧化剂,且收率良好.同时,探讨了影响反应的因素,为1,2,4-三氮唑[3,4-i]嘌呤类化合物研究奠定了基础.1,2,4-Triazolo[3,4-i]purine derivatives are potential xanthine oxidase(XO)inhibitors and expected to be used in the treatment of gout.A new one-step method for the preparation of 1,2,4-triazolo[3,4-i]purine derivatives has been reported.Seventeen novel 1,2,4-triazolo[3,4-i]purine derivatives were synthesized with 6-hydrazinyl-N9-substituted purine and aliphatic monocarboxylic acid as starting materials and anhydrous magnesium sulfate as dehydrating agent.The method is easy to operate without using other catalysts and oxidants,and the yield is good.Meanwhile,the factors affecting the reaction were discussed,which laid a foundation for the study of 1,2,4-triazolo[3,4-i]purine compounds.

关 键 词：6-肼基-N^(9)-取代嘌呤 脂肪族一元羧酸 1 2 4-三氮唑[3 4-i]嘌呤类化合物 

分 类 号：TQ460.1[化学工程—制药化工]