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作 者:陶俊阳 马文韬 王中慧 Tao Junyang;Ma Wentao;Wang Zhonghui(College of Chemistry and Chemical Engineering,Hubei University,Wuhan 430062,China)
出 处:《广东化工》2022年第20期50-52,104,共4页Guangdong Chemical Industry
摘 要:联芳基骨架广泛存在于天然产物,药物中,合成这类分子具有重要的价值。Suzuki偶联的发展为其提供了一种重要的合成方法,在此我们测试了一种新型邻位烷基化的联芳基膦在钯催化Suzuki偶联合成联芳基化合物中活性应用,能以最低0.01 mol%的钯用量以很高的产率进行反应,为合成联芳基化合物降低了成本。邻位烷基的引入有利于机理中氧化加成,还原消除步骤,与商业化膦配体对比也表现出较高的反应活性。Biaryl skeletons are widely found in natural products and medicines, and the synthesis of such molecules is of great value. The development of Suzuki coupling provides an important synthetic method. Here we tested the active application of a novel ortho-alkylated biarylphosphine in the synthesis of biaryls via palladium-catalyzed Suzuki coupling. The reaction was carried out in high yields with a minimum palladium amount of 0.01 mol%, reducing the cost for the synthesis of biaryl compounds. The introduction of vicinal alkyl groups is beneficial to the oxidative addition and reductive elimination steps in the mechanism, and also shows higher reactivity compared with commercial phosphine ligands.
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