Department of Chemistry, University of Houston, Houston, TX, 77204-5003, USA.
Department of Chemistry, University of Wrocław, 14 F. Joliot-Curie, 50-383, Wrocław, Poland.
Angew Chem Int Ed Engl. 2017 Mar 20;56(13):3630-3634. doi: 10.1002/anie.201611407. Epub 2017 Feb 24.
We have developed a method for palladium-catalyzed, pyrazole-directed sp C-H bond arylation by aryl iodides. The reaction employs a Pd(OAc) 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.
我们开发了一种钯催化、吡唑导向的 sp³ C-H 键芳基化方法,使用芳基碘化物作为底物。该反应采用 5-10 mol%负载量的 Pd(OAc)催化剂和氧化银作为卤化物去除剂,在乙酸或乙酸/六氟异丙醇溶剂中进行。吡唑部分的臭氧化反应可得到具有重要药用价值的β-苯乙胺。