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
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2017年 / 56卷 / 13期
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.
引用
收藏
页码：3630 / 3634
页数：5
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