Department of Chemistry, Dalhousie University, Halifax, Nova Scotia, Canada B3H 4J3.
J Am Chem Soc. 2011 Apr 13;133(14):5194-7. doi: 10.1021/ja200009c. Epub 2011 Mar 18.
We report the first example of selective Pd-catalyzed mono-α-arylation of acetone employing aryl chlorides, bromides, iodides, and tosylates. The use of appropriately designed P,N-ligands proved to be the key to controlling the reactivity and selectivity. The reaction affords good yields with substrates containing a range of functional groups at modest Pd loadings using Cs(2)CO(3) as the base and employing acetone as both a reagent and the solvent.
我们报道了首例使用芳基氯化物、溴化物、碘化物和对甲苯磺酸盐选择性钯催化的丙酮单α-芳基化反应。使用经过适当设计的 P,N-配体被证明是控制反应性和选择性的关键。该反应在适度的钯负载量下,使用 Cs(2)CO(3)作为碱,并使用丙酮作为试剂和溶剂,可从含有多种官能团的底物中获得良好的产率。