Patent Details

Patent ID: CN201010209723.4

Method fluoro biaryl compound is prepared in a pure aqueous solution

Description: Method fluoro biaryl compound is prepared in a pure aqueous solution, which belongs to the technical field of chemical catalysis. In this method, the halogenated aromatic compound with a fluorinated aryl boronic acid Suzuki cross-coupling method for the preparation of biaryl compounds fluoro reaction. It is a halogenated aromatic compound, an aryl boronic acid, base, catalyst and ligand in a molar ratio of 0.005 0.0025:0.001 0.5:0.75:1.0:0.0005 ~ 1 ~ 2ml of water was added, under nitrogen at 80 to 100 ℃ for 1 to 4 hours, after the completion of the reaction, the reaction mixture was added 2ml of ether extraction, phase separation was allowed to stand at room temperature, the aqueous phase containing the catalyst is recycled, the ether phase was added a saturated aqueous sodium chloride, and the reaction product was extracted with ethyl acetate. The combined organic phases, and the filtrate was concentrated and purified by column chromatography to give analytically pure fluoro biaryl compounds. The method is characterized in that the reaction is carried out in a solvent of green water, without the addition of any organic solvent; solvent system to solve the problem of water-soluble substrate reaction Africa difficulty; ligand achieved using temperature of catalyst separation and recovery of the repeat use.

Patent Details: N/A

DOI: C07B37 / 00 (2006.01) I; C07C255 / 50 (2006.01) I; C07C253 / 30 (2006.01) I; C07C25 / 18 (2006.01) I; C07C17 / 263 (2006.01) I; C07C43 / 225 (2006.01) I; C07C41 / 30 (2006.01) I; C07C49 / 813 (2006.01) I; C07C45 / 68 (2006.01) I; C07D213 / 26 (2006.01) I; C07D213 / 64 (2006.01) I; C07C13 / 28 (2006.01) I; C07C1 / 32 ( 2006.01) I; C07C22 / 08 (2006.01) I; B01J31 / 24 (2006.01) I