An Entry to a Chiral Dihydropyrazole Scaffold: Enantioselective [3 + 2] Cycloaddition of Nitrile Imines

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• 作者：Mukund P. Sibi ; Levi M. Stanley ; and Craig P. Jasperse
• 刊名：Journal of the American Chemical Society
• 出版年：2005
• 出版时间：June 15, 2005
• 年：2005
• 卷：127
• 期：23
• 页码：8276 - 8277
• 全文大小：59K
• 年卷期：v.127,no.23(June 15, 2005)
• ISSN：1520-5126

文摘

We have developed a versatile strategy to access dihydropyrazoles in highly enantioenriched form. Dipolar cycloaddition of electron-deficient acceptors and in situ-generated nitrile imines proceeds with high regio- and enantioselectivity using 10 mol % chiral Lewis acid catalyst. A variety of dihydropyrazoles that incorporate functionality for further manipulation have been prepared.