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    • 2. 发明授权
    • N-heterocyclic carbene catalyzed synthesis of N-phenylisoxazolidin-5-one derivative and synthesis of β-amino acid ester derivative
    • N-杂环卡宾催化合成N-苯基异恶唑烷-5-酮衍生物和合成β-氨基酸酯衍生物
    • US08071783B2
    • 2011-12-06
    • US12531678
    • 2008-03-14
    • Yugen ZhangJackie Y. YingJayasree SeayadPranab K. Patra
    • Yugen ZhangJackie Y. YingJayasree SeayadPranab K. Patra
    • C07D261/04C07C229/00
    • C07C227/18C07D261/04C07C229/18
    • A process for preparing a N-phenylisoxazolidin-5-one derivative is provided. The process for preparing the N-phenylisoxazolidin-5-one derivative comprises reacting an α,β-unsaturated aldehyde with nitrosobenzene in the presence of a N-heterocyclic carbene (NHC) catalyst. A process for preparing an N-alkoxyphenyl protected β-amino acid ester derivative is further provided. The process for preparing the N-alkoxyphenyl protected β-amino acid ester derivative comprises reacting an α,β-unsaturated aldehyde with nitrosobenzene in the presence of a N-heterocyclic carbene (NHC) catalyst to form a N-phenylisoxazolidin-5-one derivative, and then treating the N-phenylisoxazolidin-5-one derivative with an alcohol in the presence of an acid catalyst. A process for preparing an N-alkoxyphenyl protected β-amino acid ester derivative, comprising treating a N-phenylisoxazolidin-5-one derivative with an alcohol in the presence of an acid catalyst, is also provided.
    • 提供了制备N-苯基异恶唑烷-5-酮衍生物的方法。 制备N-苯基异恶唑烷-5-酮衍生物的方法包括在N-杂环卡宾(NHC)催化剂存在下,使α和bgr-不饱和醛与亚硝基苯反应。 还提供了制备N-烷氧基苯基保护的α-氨基酸酯衍生物的方法。 制备N-烷氧基苯基保护的α-氨基酸酯衍生物的方法包括在N-杂环卡宾(NHC)催化剂存在下使α和β-不饱和醛与亚硝基苯反应,形成N-苯基异恶唑烷-5- 一种衍生物,然后在酸催化剂存在下用醇处理N-苯基异恶唑烷-5-酮衍生物。 还提供了一种制备N-烷氧基苯基保护的氨基酸酯衍生物的方法,其包括在酸催化剂存在下用醇处理N-苯基异恶唑烷-5-酮衍生物。