【摘要】 多官能化手性氨基酸及其衍生物是一类重要的手性药物以及合成手性药的关键中间体,如现在大量用于临床的左甲状腺素、赖诺普利、阿莫西林、缬沙坦、头孢氨苄以及青霉素等。进行多官能化手性氨基酸类化合物的不对称催化合成,可为新型化学药的设计与发现开辟新的视野。噁唑烷酮(Azlactone)被证明是合成四取代氨基酸衍生物的优秀底物。可通过不对称催化手段向其中引入需要的基团,再经多取代的噁唑烷酮直接开环得到一系列的目标化合物。本文主要综述了近年来基于恶唑烷酮的不对称催化反应构建四取代氨基酸类化合物的研究。更多还原

【Abstract】 Polyfunctional chiralamino acids and their derivatives play an important role in the synthesis of chiral drugs,and are key intermediates for the synthesis of pharmaceutical compounds,such as Levothyroxine,Lisinopril,Amoxicillin,Valsar(?)an,Cefalexin,Penicillin,and so on.The asymmetric catalytic synthesis of poly functional chiralamino acids can provide new pathways for the drug design and discovery.Due to their convenient synthesis,azlactones have been proven to be valuable synthons for the synthesis of stereochemically rigid unnatural aminoacids.A series of such compounds can therefore be synthesized by ring-opening of polyfunctiona.oxazolone which was obtained by the intruction of different substitutuent to oxazolone via asymmetric catalysis.In this article,we(?)summarize the construction of polyfunctional α-amino acids via the asymmetric synthesis of oxazolone in recentyears.更多还原