(6,7-SUBSTITUTED-8-ALKOXY-1-CYCLOPROPYL-1,4-DIHYDRO-4-OXO-3-QUINOLINECARBOXYLIC ACID-03,04) BIS (ACYLOXY-0) BORATE, SALTS AND HYDRATES THEREOF

• Main Authors: MATSUKUBO, HIROSHI, FUBASAMI, HIRONOBU, TAKAGI, NAOMI
• Format: Patent
• Language: English; French
• Published: 20.07.1999
• Edition: 6
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

(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) 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, (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 (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.