Abstract
We have developed a method for palladium-catalyzed, pyrazole-directed sp(3) C-H bond arylation by aryl iodides. The reaction employs a Pd(OAc)(2) catalyst at 5-10 mol % loading and silver(I) oxide as a halide-removal agent, and it proceeds in acetic acid or acetic acid/hexafluoroisopropanol solvent. Ozonolysis of the pyrazole moiety affords pharmaceutically important β-phenethylamines.