Palladium‐Catalyzed Pyrazole‐Directed sp 3  C−H Bond Arylation for the Synthesis of β‐Phenethylamines | Zendy

Gulia Nurbey | Zendy; Daugulis Olafs | Zendy

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Palladium‐Catalyzed Pyrazole‐Directed sp 3 C−H Bond Arylation for the Synthesis of β‐Phenethylamines

Author(s) -

Gulia Nurbey,

Daugulis Olafs

Publication year - 2017

Publication title -

angewandte chemie international edition

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.831

H-Index - 550

eISSN - 1521-3773

pISSN - 1433-7851

DOI - 10.1002/anie.201611407

Subject(s) - phenethylamines , chemistry , pyrazole , acetic acid , palladium , catalysis , moiety , medicinal chemistry , solvent , aryl , halide , organic chemistry , stereochemistry , alkyl

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.

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