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Palladium-Catalyzed Pyrazole-Directed sp3 C-H Bond Arylation for the Synthesis of ?-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 ?-phenethylamines.

SUBMITTER: Gulia N 

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

REPOSITORIES: biostudies-literature

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Palladium-Catalyzed Pyrazole-Directed sp<sup>3</sup> C-H Bond Arylation for the Synthesis of β-Phenethylamines.

Gulia Nurbey N   Daugulis Olafs O  

Angewandte Chemie (International ed. in English) 20170224 13

We have developed a method for palladium-catalyzed, pyrazole-directed sp<sup>3</sup> C-H bond arylation by aryl iodides. The reaction employs a Pd(OAc)<sub>2</sub> 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. ...[more]

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