摘要
本研究开发出一条以1H-咪唑-5-甲酸(1)为起始原料,经酯化、氨化、酰化、氨解环合和氯代反应合成出2-异丙基-4-氯-咪唑并[5,1-f][1,2,4]三嗪(6)的路线,并对合成中关键步骤反应条件进行了优化:酰化、环合和氯代,对各中间体及目标产物6进行了核磁表征,6的总收率为29.2%。该方法操作简便、反应条件温和、原料价廉易得,是合成咪唑并三嗪类的简便合成路线。
In this paper, a synthetic route of imidazo-triazine compounds with simple operations and mild reaction conditions was developed. 4-chloro-2-isopropyl-imidazo [5,1-f] [1,2,4] triazine （6） was synthesized by esterification, acylation, amination cyclization and chlorination reaction. The synthesis use 1H-imidazole-5-carboxylic acid （1） as the starting material. The reaction conditions of the key steps including acylation, cyclization, and chlorination were optimized. The intermediates and the target product 6 were characterized by NMR, and the total yield of 6 was 29.2%.
作者
杨绍娟
孟令强
霍素红
Yang Shao-juan;Meng Ling-qiang;Huo Su-hong(Yanching Institute of Technology, Sanhe 065201;Yanbian University, Yanji 133002)
出处
《中国抗生素杂志》
CAS
CSCD
2018年第4期462-466,共5页
Chinese Journal of Antibiotics
基金
廊坊市科技支撑计划项目(No.2017011002)
关键词
咪唑并三嗪
合成
研究
Imidazole triazine
Synthesis
Research
