2r,4s,s,r- and 2s,4r,s,r-hydroxyitraconazole

Details 2r,4s,s,r- and 2s,4r,s,r-hydroxyitraconazole 2r,4s,s,r- and 2s,4r,s,r-hydroxyitraconazole

C - Chemistry, Metallurgy

07

D

C07D 405/14 (2006.01) A61K 31/495 (2006.01) C07D 249/12 (2006.01) C07D 405/06 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2269616

A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (S,R)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and to their use for the treatment of fungal infection are also disclosed.

L'invention concerne un procédé de préparation d'isomères optiquement purs d'hydroxy-itraconazole, en particulier les deux diastéréomères cis dioxolane du (S,R)-isomère du sec-butyl, et pour réaliser la phosphatation et la sulfatation des dérivés de ces isomères. L'invention concerne également des compositions pharmaceutiques renfermant ces composés, et leur utilisation dans le traitement de mycoses.

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