富马酸卢帕他定的合成

Synthesis of Rupatadine Fumarate

氯雷他定经碱性水解、与5-甲基烟酸缩合得8-氯-6,11-二氢-11-[1-(5-甲基烟酰基)-4-哌啶亚基]-5H-苯并[5,6]环庚烷并[1,2-b]吡啶,再经POCl3/NaBH4还原后成盐制得抗过敏药富马酸卢帕他定,总收率为28%。5-甲基烟酸可由3,5-二甲基吡啶氧化得到。

Rupatadine fumarate was synthesized from lomtadine via alkaline hydrolysis and condensation with 5-methylnicotinic acid to give 8-chloro-6,11 -dihydro- 11- [ 1 - （5-methylnicotinoyl） -4-piperidinylidene] -5H-benzo [5,6] - cyclohepta [ 1,2-b] pyridine, which was subjected to reduction by POC13/NaBH4 followed by salt formation with an overall yield of 28%. 5-Methylnicotinic acid was prepared from 3,5-1utidine by oxidation.