Direct C(sp²)–H bond functionalization of the tropone skeleton constitutes an atom-economical strategy to access substituted tropones that exist in some bioactive compounds. Herein, we report a convenient method for the preparation of 2-hydrazinotropones via C(sp²)–H bond functionalization. A variety of tropones participated in the dehydrogenative hydrazination reaction with hydrazine, delivering structurally diverse 2-hydrazinotropones in moderate to good yields with extremely high regioselectivity. This method is featured by operational simplicity and metal-free reaction conditions, thereby tolerating various functional groups.

中文翻译：

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托托酮的高区域选择性脱氢酰肼化


tropone 骨架的直接 C（sp²）-H 键官能化构成了一种原子经济策略，用于获得存在于某些生物活性化合物中的取代 tropones。在此，我们报道了一种通过 C（sp²）-H 键功能化制备 2-酰嗪基促酮的便捷方法。多种托他酮参与了与肼的脱氢肼化反应，以中等至良好的产量提供结构多样的 2-肼基托肼酮，具有极高的区域选择性。该方法的特点是操作简单和无金属反应条件，因此可以容忍各种官能团。