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建立了一锅法合成哌嗪酮取代醌类衍生物的方法.该方法以哌嗪酮烯胺酯为合成砌块,以乙腈为溶剂,醋酸作催化剂,在室温条件下,通过哌嗪酮烯胺酯1与醌类化合物2的α-C选择性烷基化反应,再经氧化脱氢简洁高效地合成了一系列结构新颖的哌嗪酮醌类衍生物3a~3l,产率70%~88%.该方法具有原料易得、合成路线简洁、产率高和操作简便等特点.
A one-pot method for the synthesis of piperazinone substituted quinone derivatives was established.Methods: Piperazinone enamino ester was used as a building block, acetonitrile as solvent and acetic acid as catalyst, at room temperature, A-C selective alkylation of amine ester 1 and quinone compound 2, and then a series of novel piperazone quinone derivatives 3a ~ 3l were synthesized simply and efficiently by oxidative dehydrogenation with a yield of 70% 88% .The method is easy to get raw materials, synthetic route is simple, high yield and easy to operate and so on.