Abstract

A facile synthesis of novel 3-functionalized pyridine derivatives has been accomplished through the reaction of 4-hydroxy-3-benzoylpyridin-2(1H)-ones and β-nitrostyrenes in the presence of catalytic amount of pyrrolidine (10 mol%). In this process, the desired products were obtained with 72–87% yields using ethanol as solvent at 80 °C for 4 h. In addition, a total of 19 examples were obtained, which exhibited the broad substrate scope of the transformation. The reaction process may involve the formation of an unstable enamine intermediate and then undergo hydrolysis to afford 4-hydroxy-3-benzoylpyridin-2(1H)-one derivatives.

摘要

通过 4-hydroxy-3-benzoylpyridin-2(1 H )-ones 和β -nitrostyrenes 在催化量的吡咯烷 (10 mol%) 存在下的反应，已经完成了新型 3-官能化吡啶衍生物的简便合成。在此过程中，使用乙醇作为溶剂在 80 °C 下 4 小时，以 72-87% 的收率获得所需产品。此外，总共获得了 19 个例子，展示了转换的广泛底物范围。反应过程可能涉及不稳定的烯胺中间体的形成，然后进行水解以提供 4-hydroxy-3-benzoylpyridin-2(1 H )-one 衍生物。