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通过一锅 Suzuki 偶联反应，然后与羧酸直接环化，合成新型二芳基[d,f][1,3]二氮杂环庚烷。

Syntheses of novel diaryl[d,f ][1,3]diazepines via one-pot Suzuki coupling followed by direct ring closure with carboxylic acids.

机构信息

The Center for Combinatorial Chemistry and Drug Discovery, The College of Chemistry and The School of Pharmaceutical Sciences, Jilin University, Changchun, 130012 Jilin, People's Republic of China.

出版信息

Mol Divers. 2012 Aug;16(3):489-501. doi: 10.1007/s11030-012-9382-1. Epub 2012 Jul 1.

DOI:10.1007/s11030-012-9382-1
PMID:22752672
Abstract

A series of novel and diverse diaryl[d,f][1,3]diazepines were designed and synthesized to expand the pharmaceutical utility of the [6,7]bicyclic molecular skeletons. The facile synthesis involved two key steps: a one-pot Suzuki coupling to construct the bi-aryl intermediates from corresponding halides, and a ring closure by direct condensation with carboxylic acids.

摘要

设计并合成了一系列新颖多样的二芳基[d,f][1,3]二氮杂环庚烷，以拓展[6,7]双环分子骨架的药用功能。该合成方法简便，包含两个关键步骤：一锅法 Suzuki 偶联，从相应的卤化物构建双芳基中间体，以及通过与羧酸直接缩合进行环化。

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