Palladium-Catalyzed Pyrazole-Directed sp³ C-H Bond Arylation for the Synthesis of β-Phenethylamines.

ABSTRACT: 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.

SUBMITTER: Gulia N 

PROVIDER: S-EPMC5480374 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature