富马酸卢帕他定的合成

Synthesis of Rupatadine fumarate

摘要: 目的合成富马酸卢帕他定并改进工艺。方法以5-甲基烟酸为起始物料，经过酯化、还原、氯化、烷基化、成盐等步骤制得富马酸卢帕他定。结果所得产物经核磁共振氢谱、质谱、红外等确证其结构，总收率为46.4%。结论该工艺安全可靠，方法简便，适合工业化生产。

Abstract: OBJECTIVE To synthesis rupatadine fumarate and optimize the reaction conditions. METHODS Rupatadine fumarate was synthesized from 5-methyl nicotinic via esterification, reduction, chlorination, alkylation and salification. RESULTS The rupatadine fumarate was synthesized with a total yield of 46.4% and its structure was confirmed by 1H-NMR, MS and IR. CONCLUSION The synthetic route is suitable for production of rupatadine fumarate in industry.