Synthesis of 1,4-diazepinone derivatives via a domino aza-Michael/SN2 cyclization of 1-azadienes with α-halogenoacetamides.,Organic & Biomolecular Chemistry

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Synthesis of 1,4-diazepinone derivatives via a domino aza-Michael/SN2 cyclization of 1-azadienes with α-halogenoacetamides.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-01-23 , DOI: 10.1039/c9ob02626f
Chunhao Yuan ₁ , Hui Zhang ₁ , Mengna Yuan ₁ , Lei Xie ₂ , Xiaoqun Cao ₁

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A novel cyclization of α-halogenoacetamides with 1-azadienes has been developed for the efficient preparation of monocyclic 1,4-diazepinones in one step under transition metal-free conditions. Various α-halogenoacetamides and 1-azadienes are well tolerated and give the desired products in good to excellent yields. This cyclization also demonstrates potential synthetic utility on a gram-scale and further transformation.

中文翻译：

通过α-卤代乙酰胺的1-氮二烯的多米诺氮杂-Michael / SN2环化反应合成1,4-二氮杂庚酮衍生物。

已经开发出一种新型的α-卤代乙酰胺与1-氮杂二烯的环化反应，可在无过渡金属条件下一步有效地制备单环1,4-二氮杂酮。各种α-卤代乙酰胺和1-氮杂二烯都具有良好的耐受性，并以良好或极好的收率提供了所需的产物。该环化还证明了在克规模和进一步转化方面的潜在合成效用。

更新日期：2020-02-13

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