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建立了以杂环烯酮缩胺(HKAs)为原料,用芳基异氰酸酯为酰化剂,实现杂环烯酮缩胺选择性酰化.通过该区域选择性反应简洁、快速地合成了一系具有潜在药理活性的酰胺类杂环烯酮缩胺化合物的方法.该方法以六元或七元环杂环烯酮缩胺1~2与芳基异氰酸酯4在1,4-二氧六环溶剂中室温下合成杂环烯酮缩胺α-碳选择性酰基化产物5~6,产率90%~98%;而五元环杂环烯酮缩胺3与芳基异氰酸酯4在1,4-二氧六环溶剂中碳酸铯催化室温下合成杂环烯酮缩胺选择性氮酰基化产物7,产率78%~93%.
A series of systems were synthesized by the selective reaction of heterocycle enone ketones (HKAs) with aryl isocyanates as the acylating agent for the selective acylation of heterocycle enones. The present invention relates to a method for the preparation of an amide-type heterocycloalkenone amine compound with potential pharmacological activity, which comprises the step of reacting a 6-membered or 7-membered heterocyclic ring ketene acetal 1-2 with aryl isocyanate 4 in 1,4-dioxane solvent The a-carbon acylated products of heterocyclic heptanone were synthesized at room temperature in 5 ~ 6, the yield was 90% ~ 98%; while the five-membered ring heterene ketoamine 3 and aryl isocyanate 4 in 1,4 - Cesium Carbonate Catalyzed Synthesis of Heterocycloalkenone Selective Nitrogenylation Products 7 at Room Temperature in 78% - 78% ~ 93%.