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

作者:Que Yonglei; Xie Yuanwei; Li Tuanjie; Yu Chenxia; Tu Shujiang; Yao Changsheng*
来源:Organic Letters, 2015, 17(24): 6234-6237.
DOI:10.1021/acs.orglett.5b03223

摘要

An N-Heterocyclic Carbene (NHC)-catalyzed oxidative formal [4 + 2] annulation of acylhydrazones with saturated carboxylic acids bearing gamma-H to assemble delta-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.

  • 出版日期2015-12-18