Patent ID: 6121491
Filing Date: 2000-09-19
Classification: A61P,C07C

Abstract:
Process for the preparation of (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methylpropan-1-ol (I) or cericlamine which consists:i)--in arylating methacrylic acid with the diazonium chloride of 3,4-dichloroaniline, prepared in situ, to obtain (+/-)2-chloro-3-(3,4-dichlorophenyl)-2-methylpropionic acid (IV), ##STR8## ii)--in aminating the acid (IV) with an amine HNR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 are independently hydrogen or methyl, to obtain an amino acid (III) ##STR9## in which M is an alkali or alkaline earth metal or else hydrogen, R.sub.1 and R.sub.2 being as defined above, theniii)--in esterifying an acid (III), then, when R.sub.1 and/or R.sub.2 are hydrogen, in methylating the amine with formaldehyde and formic acid to obtain a (+/-)3-(3,4-dichlorophenyl)-2-dimethyl-amino-2-methylpropionic acid ester(II) ##STR10## in which R is lower alkyl, then iv)--in reducing the ester (II) by a metal or organometal hydride to obtain (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methylpropan-1-ol or cericlamine (INN) of formula (I) ##STR11## and in making the addition salt with hydrochloric acid.