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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
Affiliation  

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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