Organocatalytic Asymmetric Michael Addition of 1-Acetylindolin-3-ones to 伪,尾-Unsaturated Aldehydes: Synthesis of 2-Substituted Indolin-3-ones

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• 作者：Yao-Zong Liu ; Jie Zhang ; Peng-Fei Xu ; Yong-Chun Luo
• 刊名：Journal of Organic Chemistry
• 出版年：2011
• 出版时间：September 16, 2011
• 年：2011
• 卷：76
• 期：18
• 页码：7551-7555
• 全文大小：773K
• 年卷期：v.76,no.18(September 16, 2011)
• ISSN：1520-6904

文摘

A highly efficient asymmetric Michael addition of 1-acetylindolin-3-ones to 伪,尾-unsaturated aldehydes is developed to afford 2-substituted indolin-3-one derivatives in high yields (up to 94%) with good stereoselectivities (up to 11:1 dr and 96% ee). The Michael adducts can be transformed into substituted cyclopentyl[b]indoline compounds conveniently without racemization.