摘要
报道了利巴韦林(Ribavirin)的关键中间体标题化合物的合成新方法。以3-甲基-1H-1,2,4-三唑为原料,在MnO2氧化下和尿素反应,一步转化为1H-1,2,4-三唑-3-甲酰胺。然后1H-1,2,4-三唑-3-甲酰胺在饱和HCl/MeOH中醇解,以两步60%的总收率得到标题化合物。该方法避免了传统方法中具有爆炸危险的重氮化-脱氮步骤,原料易得,步骤短,收率高,为标题化合物的合成提供了新途径。
The synthesis of 1 H-1,2,4-triazole-3-carhoxylicacid methylester which is the key intermediate of Ribavirin was developed. In the presence of MnO2 and urea, 3-methyl-1H- 1,2,4-triazole could be converted into 1H-1,2,4-triazole-3- carboxamide in good yield. The 1H-1,2,4-triazole-3-carboxamide was alcoholized in saturated HCL/MeOH solution to afford 1H-1,2,4-triazole-3-carboxylicacid methylester in high yield. The 1H-1, 2, 4-triazole-3-carboxylicacid methylester was synthesized in two steps and 60% total yield. This method takes advantages of avoiding of diazotization step, available starting materials, short steps and high yield, providing a new avenue for 1H-1,2, 4-triazole-3-carboxylicacid methylester preparation.
出处
《化学试剂》
CAS
CSCD
北大核心
2014年第9期857-858,864,共3页
Chemical Reagents
基金
河南省教育厅自然科学研究计划资助项目(2011A150018)
