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Palladium-Catalyzed Pyrazole-Directed sp3 C-H Bond Arylation for the Synthesis of β-Phenethylamines
被引:60
|作者:
Gulia, Nurbey
[1
,2
]
Daugulis, Olafs
[1
]
机构:
[1] Univ Houston, Dept Chem, Houston, TX 77204 USA
[2] Univ Wroclaw, Dept Chem, 14 F Joliot Curie, PL-50383 Wroclaw, Poland
关键词:
arenes;
C-C coupling;
C-H activation;
homogeneous catalysis;
palladium;
ALPHA-AMINO-ACIDS;
C(SP(3))-H ARYLATION;
TRACE AMINES;
ACTIVATION;
FUNCTIONALIZATION;
CYCLOPALLADATION;
ALKYLATION;
CARBON;
POSITIONS;
OXIDATION;
D O I:
10.1002/anie.201611407
中图分类号:
O6 [化学];
学科分类号:
0703 ;
摘要:
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 beta-phenethylamines.
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页码:3630 / 3634
页数:5
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