Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08903, USA.
Org Lett. 2010 Mar 5;12(5):1032-5. doi: 10.1021/ol1000318.
The development of a general and mild method for Pd-catalyzed alpha-arylation of a variety of ketones bearing multiple heteroatoms is described. The ligand to metal ratio and the position of the heteroatoms with respect to the carbonyl moiety significantly impact the efficiency of these transformations. In addition, these conditions were successfully applied to the alpha-arylation of cyclic imines. A detailed investigation of the scope of this methodology, including the effect of the ligand to metal ratio, is discussed.
描述了一种通用且温和的 Pd 催化多种含有多个杂原子的酮的α-芳基化方法。配体与金属的比例以及杂原子相对于羰基部分的位置对这些转化的效率有显著影响。此外,这些条件还成功应用于环状亚胺的α-芳基化反应。详细讨论了该方法的适用范围,包括配体与金属的比例的影响。