Palladium-Catalyzed Pyrazole-Directed sp3 C-H Bond Arylation for the Synthesis of β-Phenethylamines.
Nurbey GuliaOlafs DaugulisPublished in: Angewandte Chemie (International ed. in English) (2017)
We have developed a method for palladium-catalyzed, pyrazole-directed sp3 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.