Process and intermediates for preparing...

Details Process and intermediates for preparing... Process and intermediates for preparing...

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) C07D 209/52 (2006.01)

Patent

CA 2181351

This invention relates to novel processes for preparing compounds of formula (I), wherein R1H is as defined below, which is a salt of the naphthyridone antibiotic 7-(1.alpha.,5.alpha.,6.alpha.)-(6-amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8- naphthyridine-3-carbocylic acid and a pharmaceutically acceptable acid. The salt and antibiotics have antibacterial activity. This invention also relates to novel intermediates, and processes for their preparation, of formulae (IV), (IIIB) or (IIIA). The compounds of formulae (IIIA), (IIIB) and (IV) are useful as intermediates in the syntheses of the azabicyclo naphthyridone carboxylic acid alkanesulfonic acid salts of formula (I).

L'invention se rapporte à de nouveaux procédés de préparation de composés de la formule (I), dans laquelle R?1¿H est tel que ci-défini, un sel de l'antibiotique à base de naphtyridone, l'acide 7-(1.alpha.,5.alpha.,6.alpha.)-(6-amino-3-azabicyclo[3,1,0]hex-3-yl)-1-(2,4-difluorophényl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphtyridine-3-carboxylique, ainsi qu'un acide pharmaceutiquement acceptable. Ce sel et ces antibiotiques présentent une activité antibactérienne. L'invention se rapporte également à de nouveaux intermédiaires des formules (IIIA), (IIIB) et (IV),ainsi qu'à des procédés destinés à leur préparation. Les composés des formules (IIIA), (IIIB) et (IV) sont aptes à être utilisés comme intermédiaires dans les synthèses des sels d'acide alcanesulfonique/d'acide azabicyclo naphtyridonecarboxylique de la formule (I).

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