Novel polyhydro derivatives of tylosine and process for...

C - Chemistry – Metallurgy – 07 – H

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C07H 17/08 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2217785

The invention relates to 13-hydroxy-tylosine derivatives, novel semisynthetic antibiotics from the class of macrolides, and to a process for the preparation thereof. According to the present invention by a reductive opening of the oxirane ring of tylosine 13-hydroxy compounds are obtained, which are then subjected to a hydrogenation of the double bond and then 13-hydroxy dihydro or tetrahydro compounds are subjected to an oximation reaction or 13-hydroxy oximes are subjected to the hydrogenation of the double bond.

L'invention porte sur des dérivés de 13-hydroxytylosine, nouveaux antibiotiques semi-synthétiques de la catégorie des macrolides, et sur leur préparation. Selon l'invention, l'ouverture par réduction du cycle oxirane de la tylosine donne des composés 13-hydroxylés, qui sont ensuite soumis à une hydrogénation de la double liaison; les composés 13-hydroxy-dihydro ou -tétrahydro sont ensuite soumis à une réaction d'oximation, ou la double liaison des 13-hydroxyoximes est hydrogénée.

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