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发明公开
CN106083649A 一种3,5‑二芳基‑2,6,6‑三氰基‑1‑亚氨基‑2,4‑环己二烯衍生物的合成方法 失效 - 权利终止

一种3,5‑二芳基‑2,6,6‑三氰基‑1‑亚氨基‑2,4‑环己二烯衍生物的合成方法
摘要：
本发明公开一种3,5‑二芳基‑2,6,6‑三氰基‑1‑亚氨基‑2,4‑环已二烯衍生物的合成方法，该方法先将查耳酮衍生物与丙二腈二聚体在碱的促进下室温反应，得到相应的迈克尔加成产物，然后将迈克尔加成产物在碱的促进下发生关环和氧化脱氢反应，即可得到3,5‑二芳基‑2,6,6‑三氰基‑1‑亚氨基‑2,4‑环已二烯衍生物。与传统的方法相比，本发明的两步合成中使用了价格低廉的普通碱作为促进剂，有效降低了成本，且产物收率高，特别是在构建环已二烯衍生物中，应用这种方法，环已二烯中取代基的选择有较大的灵活性。本发明方法合成的3,5‑二芳基‑2,6,6‑三氰基‑1‑亚氨基‑2,4‑环已二烯衍生物可用于杂多环化学、天然抗生素的合成、抗癌药物的合成及天然产物结构改造研究领域。
摘要（英）：

The invention discloses synthesis method of a 3,5-diaryl-2,6,6-tricyan-1-imino-2,4-cyclohexadiene derivative. The method is as below: reacting a chalcone derivative with a malononitrile dimer under the promotion of alkali at room temperature to obtain a corresponding Michael adduct; then subjecting the Michael addition product to cyclization and dehydrogenation oxidation under the promotion of alkali to obtain the 3,5-diaryl-2,6,6-tricyan-1-imino-2,4-cyclohexadiene derivative. Compared with the traditional method, the two-step synthesis of the invention uses ordinary alkali with low price as a catalyst, so as to effectively reducing the cost and reach high product yield. Especially, in the construction of cyclohexadiene derivative, the method can realize greater flexibility in the selection of a substituent in cyclohexadiene. The 3,5-diaryl-2,6, 6-tricyan-1-imino-2,4-cyclohexadiene derivative synthesized by the method can be used in the fields of synthesis of heteropolycyclic chemical and natural antibiotics, synthesis of anticancer drug, and research on structural modification of natural products.

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