罗替戈汀合成路线综述  

Review of Synthetic Routes of Rotigotine

作　　者：胡晨 马少玲 彭璟 HU Chen;MA Shao-ling;PENG Jing(School of Chemistry and Life Science of Nanjing University Jinling College,Jiangsu Nanjing 210089,China)

机构地区：[1]南京大学金陵学院化学与生命科学学院,江苏南京210089

出　　处：《广州化工》2021年第4期6-9,共4页GuangZhou Chemical Industry

基　　金：南京大学金陵学院教学改革研究项目(001052804)。

摘　　要：帕金森病(Parkinson s disease,PD)又称“震颤麻痹”是常见的老年中枢神经系统退行性疾病,罗替戈汀(Rotigotine)是一种非麦角类选择性多巴胺受体激动剂(D 1/D 2/D 3)类药物,通过刺激体内的多巴胺受体,模拟多巴胺(神经递质)的功能以治疗帕金森病。本文分别从拆分合成、手性试剂辅助合成和立体选择合成路线三个方面论述了罗替戈汀的合成路线以及各种路线的特点,从中可以看出拆分合成和手性试剂辅助合成是目前罗替戈汀合成的主要路线。Parkinson s disease(PD),which is also called“paralysis agitans”,is the old age of common central nervous system degenerative disease.Rotigotine is a non-ergotine selective dopamine receptor agonist(D 1/D 2/D 3)that mimics the function of dopamine(neurotransmitter)by stimulating dopamine receptors in the body to treat Parkinson s disease.The synthetic route of Rotigotine and the characteristics of all kinds of routes were discussed from three aspects:resolution synthesis,chiral auxiliary synthesis and stereoselective synthesis.It can be seen that resolution synthesis and chiral auxiliary synthesis are the main routes of rotigotine synthesis at present.

关 键 词：罗替戈汀 帕金森病 拆分合成 手性试剂辅助合成 

分 类 号：R971.5[医药卫生—药品]