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通过缺电子吡咯与芳基硼酸的铜（II）介导交叉偶联轻松合成N-芳基吡咯。

Facile synthesis of N-aryl pyrroles via Cu(II)-mediated cross coupling of electron deficient pyrroles and arylboronic acids.

作者信息

Yu Shu, Saenz James, Srirangam Jayaram K

机构信息

Chemical Research and Development, Pfizer Global Research & Development-La Jolla, 3565 General Atomics Court, San Diego, California 92121, USA.

出版信息

J Org Chem. 2002 Mar 8;67(5):1699-702. doi: 10.1021/jo016131f.

DOI:10.1021/jo016131f
PMID:11871908
Abstract

N-Arylation of electron-deficient pyrroles has been achieved by cross-coupling with arylboronic acids at room temperature in the presence of stoichiometric amounts of copper(II) acetate. The generality of this reaction has been established with variously substituted pyrroles as well as boronic acids. A key intermediate in the synthesis of a matrix metalloprotease inhibitor has been achieved using this methodology.

摘要

在化学计量的醋酸铜（II）存在下，缺电子吡咯的N-芳基化反应已通过与芳基硼酸在室温下交叉偶联实现。该反应的通用性已通过各种取代的吡咯以及硼酸得以确立。使用这种方法已成功合成了一种基质金属蛋白酶抑制剂的关键中间体。

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