Jangsu Key Laboratory of Green Synthetic Chemistry for Functional Materials, School of Chemistry and Chemical Engineering, Jiangsu Normal University , Xuzhou Jiangsu 221116, P. R. China.
Org Lett. 2015 Dec 18;17(24):6234-7. doi: 10.1021/acs.orglett.5b03223. Epub 2015 Dec 8.
An N-Heterocyclic Carbene (NHC)-catalyzed oxidative formal [4 + 2] annulation of acylhydrazones with saturated carboxylic acids bearing γ-H to assemble δ-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.
N-杂环卡宾（NHC）催化酰腙与带有γ-H 的饱和羧酸的氧化形式[4+2]环加成反应，通过原位活化策略构建具有手性碳中心的δ-内酰胺。该反应的起始原料易得、对映选择性优异、反应条件温和、产率高、产物具有潜在的生物意义，因此为构建吡啶酮骨架提供了一种有吸引力的替代方法。
