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使用亚硝基芳烃实现金属自由的直接 C(sp 2 )-H 芳基化反应,得到作为多功能 Aβ 聚集调节剂的 2-羟基-二(杂)芳基胺。

Metal free direct C(sp)-H arylaminations using nitrosoarenes to 2-hydroxy-di(het)aryl amines as multifunctional Aβ-aggregation modulators.

机构信息

Department of Chemistry, Indian Institute of Technology Guwahati, 780139, India.

出版信息

Chem Commun (Camb). 2018 Dec 13;54(100):14081-14084. doi: 10.1039/c8cc08470j.

Abstract

An unprecedented metal free arylamination reaction involving nitrosoarenes as the electrophilic aminating agents is reported. The direct arylamination of a broad range of substrates, such as naphthols, hydroxyquinolines, hydroxyquinones, coumarins and 1,3-cyclohexadienones was achieved under operationally simple and mild conditions without the aid of additional reagents/steps for N-O bond reduction. Interestingly, novel 2-hydroxydiaryl amines were found to act as Aβ-aggregation inhibitors.

摘要

本文报道了首例涉及亚硝基芳烃作为亲电胺化试剂的无金属芳基胺化反应。在无需额外试剂/步骤还原 N-O 键的情况下,在操作简单温和的条件下,实现了各种底物(如萘酚、羟基喹啉、羟基对苯二酮、香豆素和 1,3-环己二烯酮)的直接芳基胺化。有趣的是,新型 2-羟基二芳基胺被发现可作为 Aβ 聚集抑制剂。

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