PROCESS FOR THE ENANTIOMERIC ENRICHMENT OF SALBUTAMOL AND SALBUTAMOL PRECURSORS

摘要

The present invention relates to a process for the enantiomeric enrichment of salbutamol and salbutamol precursors and the acid-addition salts thereof: (I) where R is hydrogen or benzyl, R' is hydrogen or benzyl and X is CH<SUB>2</SUB>OH or COO-C<SUB>1</SUB>-C<SUB>4</SUB>-alkyl the process comprising the crystallization of a compound of the formula (I) in the form of its acid-addition salt with an achiral carboxylic acid A that has at least three carbon atoms and a solubility of less than 50 g/l in water at pH < 3, 20°C and 1013 mbar, from a solution containing a mixture of the enantiomers of the compound of formula (I) and the achiral carboxylic acid A in the presence of seed crystals of the desired enantiomer of the compound of formula (I) or the acid addition salt thereof, whereby the enantiomerically enriched acid-addition salt of the compound of formula (I) is obtained.