4-甲基-2-氧代-6-芳氨基-二氢-吡喃-3-腈衍生物的合成

Synthesis of 4-Methyl-2-oxo-6-arylamino-2H-pyran-3-carbonitrile Derivatives

2-吡喃酮衍生物在药物领域表现出了巨大的应用潜力,已有很多该类骨架结构用作合成药物活性分子前体.因此,探索新型2-吡喃酮衍生物的合成方法非常重要.以β-酮酰胺衍生物和氰基乙酸乙酯为原料一步反应合成了2-吡喃酮衍生物,具有产物收率高(82%~93%)、反应条件温和产物后处理方便等优点,为2-吡喃酮生物的合成提供了新策略.

2-Pyrone derivatives have demonstrated considerable potential for usage in the field of medicine.Many of these skeleton structures have been used as precursors in the synthesis of pharmacologically active molecules.As a result,it is critical to explore new approaches for the synthesis of 2-pyrones.A series of 2-pyrone derivatives were synthesized fromβ-oxo amides and ethyl cyanoacetate through one-step reaction.The methodology offers several significant advantages including mild conditions,ease of handling,and high yields(82%~93%).Such,an efficient synthesis approach for 2-pyrones is provided.