新型2-吡啶酮衍生物的无催化剂合成

Catalyst-free Synthesis of Novel 2-Pyridinone Derivatives

以3-烯基氧化吲哚/苯并呋喃酮-色酮合成子1为原料,在无催化剂作用下,与各种脂肪伯胺或者醋酸铵2发生开环和重新关环反应,获得了15个未见文献报道的新型2-吡啶酮衍生物3a~3o,产率为73%~93%,其结构经^(1)H NMR,^(13)C NMR和HR-MS(ESI-TOF)表征,通过单晶进一步确定了化合物3e的构型。该类化合物含有2-羟基苯甲酰基和2-吡啶酮生物活性骨架,在医药行业有一定应用价值。

In this paper,3-vinyl oxindole/benzofuranone-chromone synthons 1 and various primary aliphatic amines or ammonium acetate 2 were used as raw materials,the ring opening and recyclization reaction occurred.Fifteen novel 2-pyridinone derivatives 3a~3o were obtained.The yields of 3a~3o were 73%~93%.The structures of products 3 were characterized by ^(1)H NMR,^(13)C NMR and HR-MS(ESI-TOF).The configuration of compound 3e was further determined by single crystals.These compounds contain two potential bioactive skeletons:2-hydroxy benzoyl group and 2-pyridinone,which have important potential value for the pharmaceutical industry.