Acid-Mediated N–H/α,β-C(sp3)–H Trifunctionalization of Pyrrolidine: Intermolecular [3 + 2] Cycloaddition for the Construction of 2,3-Dihydro-1H-Pyrrolizine Derivatives
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- 作者：Kai-Lu Zheng ; Wen-Ming Shu ; Jun-Rui Ma ; Yan-Dong Wu ; An-Xin Wu
- 刊名：Organic Letters
- 出版年：2016
- 出版时间：August 5, 2016
- 年：2016
- 卷：18
- 期：15
- 页码：3526-3529
- 全文大小：362K
- 年卷期：0
- ISSN：1523-7052
文摘
A one-pot acid-mediated reaction has been developed for the N–H/α,β-C(sp3)–H trifunctionalization of pyrrolidine without any metallic reagents or external oxidants. This reaction involves the intermolecular [3 + 2] cycloaddition of in situ-generated azomethine ylides with acrylic esters to provide facile access to 2,3-dihydro-1H-pyrrolizine derivatives in high yields under mild conditions.