钯催化的未保护五元杂环溴化物的氨化反应。
Palladium-catalyzed amination of unprotected five-membered heterocyclic bromides.
机构信息
Department of Chemistry, Massachusetts Institute of Technology , Cambridge, Massachusetts 02139, United States.
出版信息
Org Lett. 2014 Feb 7;16(3):832-5. doi: 10.1021/ol4035947. Epub 2014 Jan 13.
Abstract
An efficient method for the palladium-catalyzed amination of unprotected bromoimidazoles and bromopyrazoles is presented. The transformation is facilitated by the use of our newly developed Pd precatalyst based on the bulky biarylphosphine ligand tBuBrettPhos (L4). The mild reaction conditions employed allow for the preparation of a broad scope of aminoimidazoles and aminopyrazoles in moderate to excellent yields.
摘要
本文提出了一种高效的钯催化未保护的溴代咪唑和溴代吡唑的氨化方法。该转化通过使用我们新开发的基于大位阻联芳基膦配体 tBuBrettPhos（L4）的 Pd 前催化剂来促进。所采用的温和反应条件允许在中等至优异的产率下制备广泛的氨基咪唑和氨基吡唑。
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