卢帕他定中间体5-甲基烟酸的合成  

Synthesis of 5-Methylnicotinic Acid as an Intermediate of Rupatadine

作　　者：倪生良[1] 

机构地区：[1]湖州师范学院生命科学院,湖州313000

出　　处：《内蒙古石油化工》2007年第8期20-21,共2页Inner Mongolia Petrochemical Industry

基　　金：浙江省湖州市科技局项目(2006YG21)

摘　　要：以3,5-二甲基吡啶为原料,用高锰酸钾选择性氧化,合成抗过敏性药物卢帕他定中间体5-甲基烟酸。经正交化试验,其合成最佳工艺是:n(3,5-二甲基吡啶)∶n(KM nO4)=1∶1.8,反应温度45℃,反应时间3h。反应收率62%,HPLC大于99%,产物经IR表征。5- methylnicotinic acid as a intermediate of rupatadine , was synthesized from 3, 5- dimethylpyridine by the reaction of sective oxidation with KMnO4. The reaction conditions were optimized with the orthogonal matrix. The most favorite technological conditions were： n（3,5-dimethylpyridine ）：n （KMnO4）=1：1. 8, 45℃ and 3h. The yield of product was 62%, HPLC was beyond 99%. The structure was characterized by IR.

关 键 词：5-甲基烟酸 3.5-二甲基毗啶 合成 

分 类 号：TQ460.4[化学工程—制药化工]