Method for producing n-methylnaltrexone bromide
AssigneeCilag AG
InventorsUlrich Weigl, Pascal Schär, Alfred Stutz
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Abstract
Process for the preparation of N-methylnaltrexone bromide, wherein a compound of the general formula (I): wherein X− represents an anion other than the bromide anion, and R represents hydrogen or a leaving group, is dissolved or dispersed in a suitable polar solvent, the solution or dispersion is mixed with a compound containing bromide anions, and the resulting reaction mixture is stirred until N-methylnaltrexone bromide has formed and crystallised, wherein, in the case where R represents a leaving group, that group is removed during or after the reaction.
Claims19
Process for the preparation of N-methylnaltrexone bromide, characterised in that a compound of the general formula (I):
- wherein
- X− represents an anion other than the bromide anion, and
- R represents hydrogen or a leaving group,
- (i) is dissolved or dispersed in a suitable polar solvent, (ii) the solution or dispersion is mixed with a compound containing bromide anions, and the resulting reaction mixture is stirred until N-methylnaltrexone bromide has formed and crystallised, wherein, in the case where R represents a leaving group, that group is removed during or after the reaction.
Dependencies are inferred from the claim text.