A novel palladium-catalyzed intramolecular hydroaminocarbonylation of aminoalkynes has been developed. This direct and operationally simple protocol provides a rapid and reliable approach to a diverse array of valuable seven- and eight-membered lactams with high chemoselectivity and regioselectivity. The high selectivity might be attributed to rational tuning the electronic nature of the amine moiety and the palladium catalyst, which enabled this transformation to proceed in the absence of acidic or any other additives under fairly mild reaction conditions. This method paves the way for the synthesis of medium-sized lactams.

中文翻译：

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钯催化氨基炔烃分子内氢氨基羰基化反应选择性构建中型内酰胺

已经开发了一种新型的钯催化的氨基炔烃分子内氢氨基羰基化反应。这种直接且操作简单的方案为具有高化学选择性和区域选择性的有价值的七元和八元内酰胺的多样化阵列提供了一种快速可靠的方法。高选择性可能归因于对胺部分和钯催化剂的电子性质的合理调节，这使得该转化能够在相当温和的反应条件下在不存在酸性或任何其他添加剂的情况下进行。该方法为中型内酰胺的合成铺平了道路。