Process for the preparation of aryl-pyridinyl compounds
US6765097B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 11, 2002 |
| Grant date | Jul 20, 2004 |
| Priority date | — |
| Expiry date | Jun 7, 2022 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D405/10
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.