发明名称 Process for the preparation of aryl-pyridinyl compounds
摘要 A process is described for the preparation of arylpyridine compounds by aryl-aryl cross-coupling reactions between a halopyridine and an arylmagnesium halide carried out in the presence of a catalytic amount of a zinc salt and a catalytic amount of palladium. The zinc salt is preferably selected from ZnCl2, ZnBr2 and/or Zn(OAc)2, while the palladium is preferably used in the form of Pd(PPh3)4 or Pd(OAc)2 +4 PPh3. The reaction can also be carried out in the presence of bidentate phosphines, such as, for example, 1,3-bis(diphenylphosphine)propane or 1,4-bis(diphenylphosphine)-butane. It is thus possible to obtain molar yields higher than 97% (calculated relative to the halopyridine) and a catalyticity of more than 2000.
申请公布号 US6765097(B1) 申请公布日期 2004.07.20
申请号 US20020110685 申请日期 2002.04.11
申请人 EUTICALS PRIME EUROPEAN THERAPEUTICAL SPA 发明人 GIORDANO CLAUDIO;POZZOLI CLAUDIO;BENEDETTI FABIO
分类号 C07D213/48;C07D213/53;C07D405/10;(IPC1-7):C07D213/46 主分类号 C07D213/48
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