C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 5/04 (2006.01)
Patent
CA 2046361
(6,7-Substituted-8-alkoxy-1-cyclopropyl-1,4-dihydro-4- oxo-3-quinolinecarboxylic acid-O3,O4) bis (acyloxy-O) borate, and salts and hydrates thereof, represented by the general formula (I) Image wherein X denotes a halogen atom; R denotes an aliphatic acyloxy group having 2 - 6 carbon atoms, aliphatic acyloxy group having 2 - 6 carbon atoms optionally substituted with a halogen atom, or aromatic acyloxy group having 7 - 11 carbon atoms; R1 denotes a lower alkyl group; R2 denotes a hydrogen atom, halogen atom, amino group or nitro group; Z denotes a halogen atom, Image (wherein n is 1 or 2; R3 denotes hydrogen atom; a lower alkyl group, acyl group, alkoxycarbonyl group or aralkyl group; R4 and R5 each independently denote a hydrogen atom, lower alkyl group, substituted lower alkyl group, cycloalkyl group or phenyl group respectively) or Image (wherein k is 0, 1 or 2; ~ is 0, 1 or 2; m is 0 or 1; R6 denotes a hydrogen atom, halogen atom, lower alkyl group or hydroxyl group; R7 denotes a hydrogen atom, lower alkyl group or substituted lower alkyl group; R8 denotes a hydrogen atom, lower alkyl group, acyl group, alkoxycarbonyl group or aralkyl group) or an azetidino group, pyrrolidino group, 3-hydroxypyrrolidino group, piperidino group, morpholino group or thiomorpholino group. These compounds are especially useful in the preparation of quinolonecarboxylic compounds which are useful as medicaments.
Fubasami Hironobu
Matsukubo Hiroshi
Takagi Naomi
Borden Ladner Gervais Llp
Kyorin Pharmaceutical Co. Ltd.
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