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无需过渡金属的芳基溴代物的硼化反应:使用简单的二硼源。

Transition-Metal-Free Borylation of Aryl Bromide Using a Simple Diboron Source.

机构信息

Department of Chemistry, Gwangju Institute of Science and Technology (GIST), Gwangju 61005, Republic of Korea.

出版信息

J Org Chem. 2020 Aug 21;85(16):10966-10972. doi: 10.1021/acs.joc.0c01065. Epub 2020 Aug 10.

Abstract

In this study, we developed a simple transition-metal-free borylation reaction of aryl bromides. Bis-boronic acid (BBA), was used, and the borylation reaction was performed using a simple procedure at a mild temperature. Under mild conditions, aryl bromides were converted to arylboronic acids directly without any deprotection steps and purified by conversion to trifluoroborate salts. The functional group tolerance was considerably high. The mechanism study suggested that this borylation reaction proceeds via a radical pathway.

摘要

在这项研究中,我们开发了一种简单的过渡金属免费芳基溴的硼化反应。使用双硼酸(BBA),并在温和的温度下通过简单的程序进行硼化反应。在温和的条件下,芳基溴直接转化为芳基硼酸,无需任何脱保护步骤,并通过转化为三氟硼酸盐盐进行纯化。官能团耐受性相当高。机理研究表明,该硼化反应通过自由基途径进行。

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