一步法合成1,2,4-三氮唑[3,4-i]嘌呤类化合物
收稿日期: 2021-10-08
修回日期: 2022-01-26
网络出版日期: 2022-02-10
基金资助
国家自然科学基金(U1604283); 国家科技重大专项(2014ZX09J14101-01A); 洛阳市科技计划医疗卫生(1720001A-8)
One-Step Synthesis of 1,2,4-Triazolo[3,4-i]purine Derivatives
Received date: 2021-10-08
Revised date: 2022-01-26
Online published: 2022-02-10
Supported by
National Natural Science Foundation of China(U1604283); National Science and Technology Major Project(2014ZX09J14101-01A); Medical and Health Project of Luoyang Science and Technology Plan(1720001A-8)
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-N9-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.
楚治良 , 陈晖娟 , 单帅 , 王晓娜 , 高春芳 , 渠桂荣 , 刘忠于 , 郭海明 . 一步法合成1,2,4-三氮唑[3,4-i]嘌呤类化合物[J]. 有机化学, 2022 , 42(5) : 1551 -1556 . DOI: 10.6023/cjoc202110007
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
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