Ligand-Free Palladium-Catalyzed Direct Arylation of Thiazoles at Low Catalyst Loadings
Ligand-Free Palladium-Catalyzed Direct Arylation of Thiazoles at Low Catalyst Loadings
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DOI：
10.1021/jo802360d
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发表时间：
2009-02-06
影响因子：
3.6
通讯作者：
Doucet, Henri
中科院分区：
文献类型：
--
作者：
Roger, Julien;Pozgan, Franc;Doucet, Henri
发现无配体的Pd(OAc)(2)在很低的催化剂浓度下能非常有效地催化噻唑类化合物的直接芳基化反应。使用活化的芳基溴化物，只需0.1-0.001摩尔%的催化剂即可进行该反应。有了这样的基质，这一过程在经济和环境上都很有吸引力。另一方面，在更具挑战性的底物存在的情况下，例如一些强烈失活或高度拥塞的芳基溴化物，在某些情况下，获得了令人失望的结果。
Ligand-free Pd(OAc)(2) was found to catalyze very efficiently the direct arylation of thiazole derivatives under very low catalyst concentration. By using activated aryl bromides, the reaction can be performed employing as little as 0.1-0.001 mol % catalyst. With such substrates, this procedure is economically and environmentally attractive. On the other hand, in the presence of more challenging substrates, such as some strongly deactivated or highly congested aryl bromides, in some cases, disappointing results were obtained.