Copper-Promoted 6-endo-trig Cyclization of β,γ-Unsaturated Hydrazones for the Synthesis of 1,6-Dihydropyridazines,Organic Letters

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Copper-Promoted 6-endo-trig Cyclization of β,γ-Unsaturated Hydrazones for the Synthesis of 1,6-Dihydropyridazines
Organic Letters ( IF 4.9 ) Pub Date : 2018-05-23 00:00:00 , DOI: 10.1021/acs.orglett.8b01240
Yong-Qiang Guo ₁ , Mi-Na Zhao ₁ , Zhi-Hui Ren ₁ , Zheng-Hui Guan ₁

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A novel and efficient strategy for the synthesis of 1,6-dihydropyridazines via copper-promoted 6-endo-trig cyclization of readily available β,γ-unsaturated hydrazones have been developed. A series of 1,6-dihydropyridazines have been synthesized by this method with good yields, high functional group tolerance, and remarkable regioselectivity under mild conditions. Importantly, the 1,6-dihydropyridazines can be efficiently converted to biologically important pyridazines in the presence of NaOH.

中文翻译：

铜促进的β，γ-不饱和Hy的6-内-trig环化反应合成1,6-二氢哒嗪

已经开发了通过铜促进的6 - β-内-trig环化容易获得的β，γ-不饱和酮合成1,6-二氢哒嗪的新颖而有效的策略。通过该方法合成了一系列1,6-二氢哒嗪，具有良好的收率，较高的官能团耐受性以及在温和条件下的显着区域选择性。重要的是，在NaOH的存在下，可以将1，6-二氢哒嗪有效地转化为生物学上重要的哒嗪。

更新日期：2018-05-23

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