Purification of posaconazole and of posaconazole intermediates

摘要

The present invention relates to a process for the preparation of a hydrogen chloride (HCl) salt of a compound of formula (I) wherein Y1 and Y2 are independently F or Cl, preferably F, said compound of formula (I) containing the cis-isomer and the trans-isomer, wherein the process comprises (1) providing the compound of formula (I) comprised in a first suitable solvent; and (2) treating the compound of formula (I) comprised in the first suitable solvent with HCl comprised in a second suitable solvent to obtain the HCl salt of the compound of formula (I).;

主权项

1. A process for the preparation of a hydrogen chloride (HCl) salt of a compound of formula (I) wherein Y1 and Y2 are independently F or Cl, said compound of formula (I) containing the cis-isomer of formula (II) and the trans-isomer of formula (III) the process comprising (1) providing the compound of formula (I) comprised in a first solvent; (2) treating the compound of formula (I) comprised in the first solvent with HCl comprised in a second solvent to obtain the HCl salt of the compound of formula (I); after (2), at least partially crystallizing the HCl salt of compound of formula (I); (2b) separating the at least partially crystallized HCl salt of compound of formula (I); and (3) subjecting the at least partially crystallized HCl salt of compound of formula (I) to solid extraction in a solvent to obtain the HCl salt of compound of formula (I), thereby increasing the content with regard to the HCl salt of the cis-isomer of formula (II), wherein the at least partially crystallized HCl salt of compound of formula (I) obtained from (3) contains at least 97% of the HCl salt of the cis-isomer of formula (II) and at most 3% of the HCl salt of the trans-isomer of formula (III).