匹莫范色林的合成

Synthesis of Pimavanserin

对羟基苯甲醛和异丁基溴为起始原料经过取代、正向肟化、加氢等合成4-异丁氧基苄胺,再与4-氟苄胺和N-甲基-4-哌啶酮经还原胺化反应合成的N-(4-氟苄基)-N-1-甲基哌啶胺反应得到匹莫范色林,总收率达到64%。合成方法反应条件温和,成本低廉,安全环保。

In this paper,pimavanserin is synthesized by 4-Isobutoxybenzylamine and N-(4-fluoro benzyl)-N-1-methyperidol.4-isobutylbenzaldehyde and isobutylbromine are selected as starting materials to synthesize 4-Isobutoxybenzylamine and its acetate through substitution,forward oxime and hydrogenation.N-(4-fluoro benzyl)-N-1-methyperidol is synthesized by condensation reaction with N-methyl-4-piperidine and 4-flubenzylamine as raw materials.and the reaction rate reached 64%.The synthesis method in this paper has the advantages of mild reaction conditions,low cost,safety and environmental protection.