The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).
如附图所示,本发明涉及一种制备式 I 的 N-(5-甲基烟酰基)-
4-羟基哌啶的改进型工业优势工艺。该化合物是合成鲁帕他定的关键中间体,鲁帕他定是
组胺和血小板活化因子(PAF)的强效双重拮抗剂。