过渡金属催化手性α-取代丙酸类药物的不对称氢化合成进展  

Progress of Synthesis α-Substituted Propanoic Acids Drugs by Transition Metal-catalyzed Asymmetric Hydrogenation

作　　者：李静[1] 申杰峰[1] 夏超[1] 王彦兆 刘德龙[1] 

机构地区：[1]上海交通大学药学院,上海200240

出　　处：《现代生物医学进展》2017年第25期4993-4996,共4页Progress in Modern Biomedicine

基　　金：国家自然科学基金项目(21172143)

摘　　要：手性α-取代丙酸及其衍生物是一类重要的有机合成彻块和关键中间体,现已被广泛地应用于手性药物的合成之中。如临床正在大量使用的非甾体类抗炎药布洛芬、萘普生、酮洛芬和氟比洛芬等。众所周知的抗疟药青蒿素,其合成关键中间体二氢青蒿酸同样属于此种结构。所以,手性α-取代丙酸及其衍生物的不对称合成一直是科学家研究的热点。不对称催化氢化反应因为其原子经济性和高效性,越来越引起人们的关注。本文主要综述了近年来过渡态金属催化氢化合成手性α-取代丙酸类药物的研究进展。Optically pure α-substituted propanoic acids and their derivatives represent as an important kind of organic building blocks and key intermediates,which has been widely used in the synthesis of chiral drugs.Some of them have been used directly as nonsteroidal anti-inflammatory drugs （NSAIDs）,such as ibuprofen,naproxen,ketoprofen and so on.Dihydroartemisinic acid （DHAA）,the same structure as the α-substituted propanic acids,is a key intermediate for the synthesis of artemisinin,the most effective and current used anti-malarial drug.Therefore,the asymmetric synthesis of α-substituted propanoic acids is always a hot topic for chemical scientists.Asymmetric catalytic hydrogenation attracts more and more attentions because of its atom economy and efficiency.This dissertation will disclose the asymmetric synthesis of α-substituted propanoic acids using transition metal-complex as a chiral catalyst.

关 键 词：α-取代丙酸 手性药物 不对称催化 合成 

分 类 号：R914[医药卫生—药物化学] O621.25[医药卫生—药学]