Synthesis Process Research Of 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)? Piperazine-?1 Agonists SA4503

An agonist of ?-1 receptor,1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine(SA4503,development by Senten Pharmaceutical Co.,Ltd.),was used as an antidepressive drug.It had been progressed into clinical phase III trial at EU and been deemed to the most effective drug for antidepressive.This compound has a very broad prospect.Only one synthesis route was reported of this compound.This study designed a new synthetic route of SA4503: select 2,3-dimethoxyphenyl acetic acid and benzoic acid as raw material,reacted with thionyl chloride to prepare of the corresponding of acetyl chlorides respectively,after two steps of acylation reaction with piperazine,the obtained target di-amid intermediate was reduced by lithium aluminium hydride and acidification with HCl to give(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine hydrochlorid(SA4503).This method is simply and can be used to industrialization.