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芳杂环硼酸(1.2倍摩尔量)在Pd Cl2(15%mol)、PPh3(200%mol)和Ag2O(200%mol)催化下与磷酸酯于N,N-二甲基苯胺中100℃反应2 h,可以生成相应的C-P偶联产物芳杂环膦酸酯,19例收率51%~95%。杂环上连有给电子基团比吸电子基团收率高,连有较大位阻基团则难反应;不同的磷酸酯在该反应条件下能得到中等至较好收率,但磷酸二甲酯反应很
The aromatic heterocyclic boronic acids (1.2-fold molar amount) were reacted with phosphoric acid ester at 100 ℃ in N, N-dimethylaniline under the catalysis of Pd Cl2 (15% mol), PPh3 (200% mol) and Ag2O 2 h, can generate the corresponding CP coupling products aromatic heterocyclic phosphonate, 19 cases of 51% to 95% yield. The number of electron donating groups on the heterocyclic ring is higher than that on the electron-withdrawing group, and even the more hindered groups are difficult to react. Different phosphates can get moderate to good yield under the reaction conditions, Dimethyl reaction is very