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Oxidation of diazenyl-protected N-heterocycles – a new entry to functionalized lactams

机译:二氮烯基保护的N-杂环的氧化-功能化内酰胺的新进入

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Functionalized lactams are an important class of heterocycles since they are useful intermediates in organic synthesis and show biological activity in diverse therapeutic applications. In the herein presented study, a strategy for the synthesis of N-aryldiazenyllactams, offering the direct access to protected lactam derivatives is described. After the formation of triazenes from diazonium salts and commercially available N-heterocycles, oxidation (directed CH activation) with periodate under ruthenium catalysis furnished N-diazenyllactams in one step. To demonstrate the suitability of the resulting lactams for further functionalizations, the alkylation of a N-diazenyllactam is presented for one example.
机译:官能化内酰胺是一类重要的杂环,因为它们是有机合成中的有用中间体,并在各种治疗应用中显示出生物学活性。在本文提出的研究中,描述了用于合成 N -芳基二氮烯基内酰胺的策略,该策略提供了直接进入受保护的内酰胺衍生物的途径。由重氮盐和市售的N-杂环形成三氮烯后,在钌催化下用高碘酸盐氧化(定向CH活化)一步即可得到 N -二氮烯基内酰胺。为了证明所得内酰胺对进一步官能化的适用性,给出了一个 N -二氮烯基内酰胺的烷基化实例。

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