| 韦萱 王建霞 李静 夏超 刘德龙△.基于噁唑烷酮的不对称催化合成构建多官能化手性氨基酸类化合物[J].现代生物医学进展英文版,2016,16(20):3992-3997. |
| 基于噁唑烷酮的不对称催化合成构建多官能化手性氨基酸类化合物 |
| The Construction of Polyfunctional Chiral Amino Acids via AsymmetricCatalysis of Oxazolone |
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| DOI： |
| 中文关键词: 噁唑烷酮 手性代氨基酸 不对称催化 合成 |
| 英文关键词: Azlactone Chiral alpha-amino acids Asymmetric catalysis Synthesis |
| 基金项目:国家自然科学基金项目（21172143） |
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| 中文摘要: |
| 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。 |
| 英文摘要: |
| Polyfunctional chiral amino 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, Valsartan, Cefalexin,
Penicillin, and so on. The asymmetric catalytic synthesis of polyfunctional chiral amino 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 amino acids. A series of such compounds can therefore be synthesized by ring-opening of polyfunctional
oxazolone which was obtained by the intruction of different substitutuent to oxazolone via asymmetric catalysis. In this article, we'll
summarize the construction of polyfunctional alpha-amino acids via the asymmetric synthesis of oxazolone in recent years. |
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