PROCESS FOR THE PREPARATION OF (+/-)3-(3,4-DICHLOROPHENYL)-2-DIMETHYLAMINO-2-METHYLPROPAN-1-OL OR CERICLAMINE (INN) AND INTERMEDIATES THEREOF

摘要

PCT No. PCT/EP98/02213 Sec. 371 Date Dec. 20, 1999 Sec. 102(e) Date Dec. 20, 1999 PCT Filed Apr. 6, 1998 PCT Pub. No. WO98/45248 PCT Pub. Date Oct. 15, 1998Process for the preparation of cericlamine which consists: i) in arylating methacrylic acid with the diazonium chloride of 3,4-dichloroaniline, to obtain (+/-)2-chloro-3-(3,4-dichlorophenyl)-2-methylpropionic acid, ii) in aminating the acid with dimethylamine, to obtain (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methylpropionic acid, or an alkaline metal salt thereof, iii) in esterifying the amino-acid or its salt, then, iv) in reducing the ester by a metal or organometal hydride to obtain (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methyl-propan-1-ol.