Pastine Stefan J, Gribkov Denis V, Sames Dalibor
Department of Chemistry, Columbia University, 3000 Broadway, New York, New York 10027, USA.
J Am Chem Soc. 2006 Nov 8;128(44):14220-1. doi: 10.1021/ja064481j.
A new ruthenium-catalyzed direct sp3 C-H to C-C bond transformation is disclosed. Specifically, a method for the alpha-arylation of cyclic amines, containing either permanent (pyridine, pyrimidine) or removable (amidine) directing groups, is described. This cross-coupling reaction involves heating amine substrates with arylboronate ester at 150 degrees C in a ketone solvent with a catalytic amount of ruthenium carbonyl [Ru3(CO)12]. Arylboronate esters containing either electron-withdrawing or electron-donating substituents could be efficiently coupled. Heteroarene boronates were also effective donors.
公开了一种新型钌催化的直接sp3碳氢键到碳碳键的转化反应。具体而言，描述了一种用于环状胺α-芳基化的方法，该环状胺含有永久性（吡啶、嘧啶）或可去除（脒）导向基团。这种交叉偶联反应涉及在酮溶剂中，于150℃下将胺底物与芳基硼酸酯以及催化量的羰基钌[Ru3(CO)12]一起加热。含有吸电子或供电子取代基的芳基硼酸酯都能有效偶联。杂芳基硼酸酯也是有效的供体。
