卢帕他定的合成

Synthesis of Rupatadine

2-氰基-3-甲基吡啶经Ritter反应、烷基化、氰化、水解后闭环制得8-氯-5,6-二氢苯并[5,6]环庚[1,2-b]吡啶-11-酮,再与3-(4-氯哌啶-1-基甲基)-5-甲基吡啶经Grignard反应和脱水反应制得卢帕他定,总收率18.7%。

Rupatadine was synthesized from 2-cyano-3-methylpyridine by Ritter reaction, alkylation, cyanidation, hydrolysis and cyclization to give 8-chloro-5,6-dihydrobenzo [5,6] cyclohepta [ 1,2-b] pyridine-11-one, which was subjected to Grignard reaction and then dehydration with an overall yield of 18.7 %.