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建立了以杂环烯酮缩胺为原料与含氟β-二羰基化合物在酸性条件下“一步法”合成含氟双环吡啶类化合物的方法.以含氟β-二羰基化合物三氟乙酰乙酸乙酯(2)、六氟乙酰丙酮(3)为砌块在1,4-二氧六环溶剂中,醋酸催化下分别与杂环烯酮缩胺1反应,“一步法”简捷高效地合成了一系列新的含氟双环吡啶类化合物4a~4e及5a~5e,产率79%~95%.该方法具有原料易得、合成路线简捷、产率高、后处理简单等优点.
A method for the synthesis of fluorinated bicyclic pyridines with heterocycle enone ketones as starting materials and fluorine-containing β-dicarbonyl compounds under acidic condition was developed. The fluorinated β-dicarbonyl compounds trifluoroacetyl Ethyl acetate (2), hexafluoroacetylacetone (3) as a block in 1,4-dioxane solvent, respectively, with acetic acid catalytic reaction with heterocycle enone 1, “one-step ” simple A series of novel fluorinated bicyclic pyridines 4a ~ 4e and 5a ~ 5e were synthesized efficiently with the yield of 79% ~ 95%. The method has the advantages of easy to obtain raw materials, simple synthesis route, high yield and simple post-treatment .