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铜催化氮原子相邻的sp3 C-H键的酰胺化反应。

Copper-catalyzed amidation of sp3 C-H bonds adjacent to a nitrogen atom.

作者信息

Zhang Yongming, Fu Hua, Jiang Yuyang, Zhao Yufen

机构信息

Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, PR China.

出版信息

Org Lett. 2007 Sep 13;9(19):3813-6. doi: 10.1021/ol701715m. Epub 2007 Aug 16.

Abstract

We have developed a novel copper-catalyzed amidation of unactivated sp(3) C-H bonds adjacent to a nitrogen atom by using an inexpensive catalyst-oxidant (CuBr/(t)BuOOH) system under mild conditions. The dephenylation was first found for N-benzylaniline, and the new class of products provide diverse structures for pharmaceuticals and combinatorial chemistry.

摘要

我们开发了一种新型的铜催化的与氮原子相邻的未活化sp(3) C-H键的酰胺化反应,该反应在温和条件下使用廉价的催化剂-氧化剂(CuBr/(t)BuOOH)体系。首次发现N-苄基苯胺发生了脱苯基反应,这类新型产物为药物和组合化学提供了多样的结构。

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