多取代2,3-二氢-4-吡啶酮的水相合成

Synthesis of Polysubstituted 2,3-Dihydropyridin-4(1H)-one in Water

首次探讨了α-烯酰基二硫缩烯酮与胺的[5C+1N]水相环合反应,成功地实现多取代2,3-二氢-4-吡啶酮的水相合成.研究表明,在回流水中,(E)-2-(二乙硫基)亚甲基-3-羰基-5-芳基-N-芳基戊-4-烯酰胺1和有机胺2有效地发生[5C+1N]水相环合反应,以较好产率合成多取代2,3-二氢-4-吡啶酮3.

For the first time,the aqueous[5C+1N]annulation ofα-alkenoyl ketene dithioacetals and amines for the synthesis of polysubstituted 2,3-dihydropyridin-4(1H)-ones was developed.In boiling water,[5C+1N]annulation of(E)-2-(bis(ethylthio)methylene)-3-oxo-N,5-diarylpent-4-enamides 1 and organic amines 2 smoothly occurred,and polysubstituted 2,3-dihydropyridin-4(1H)-ones 3 was obtained in moderate yields.