|
|||||
|
|
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. |
| Keywords: | Arene C-C-Kupplung C-H-Aktivierung Homogene Katalyse Palladium |