An N-Heterocyclic Carbene-Catalyzed Oxidative 纬-Aminoalkylation of Saturated Carboxylic Acids through in Situ Activation Strategy: Access to 未-Lactam

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• 作者：Yonglei Que ; Yuanwei Xie ; Tuanjie Li ; Chenxia Yu ; Shujiang Tu ; Changsheng Yao
• 刊名：Organic Letters
• 出版年：2015
• 出版时间：December 18, 2015
• 年：2015
• 卷：17
• 期：24
• 页码：6234-6237
• 全文大小：368K
• ISSN：1523-7052

文摘

An N-Heterocyclic Carbene (NHC)-catalyzed oxidative formal [4 + 2] annulation of acylhydrazones with saturated carboxylic acids bearing 纬-H to assemble 未-lactams featuring a chiral carbon stereogenic center was developed through an in situ activation strategy. The ready availability of the starting materials, excellent enantioselectivity, facile assembly, high yields, and potential biological significance of the final products make this protocol an attractive alternative for the construction of the pyridinone scaffold.