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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。
Multifunctional chiral amino acids and their derivatives are a class of important chiral drugs and key intermediates for the synthesis of chiral drugs such as levothyroxine, lisinopril, amoxicillin, Tanzania, cephalexin and penicillin and so on. Asymmetric catalytic synthesis of multifunctional chiral amino acids can open up new horizons for the design and discovery of new chemical drugs. Azlactone proved to be an excellent substrate for the synthesis of tetrasubstituted amino acid derivatives. A series of target compounds can be directly opened by oxazolidinone by asymmetric catalysis. This review summarizes the recent studies on the construction of tetrasubstituted amino acids based on the oxazolidinone asymmetric catalysis.