| 摘要 |
Process for the preparation of 1-cyclopropyl-6-fluoro- 1,4-dihydro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept- 2-yl]-4-oxo-3-quinoline carboxylic acid and its salts. It is characterized by the treatment of a C1-C4 alkyl 1- cyclopropyl-6-fluoro-7-chloro-1,4-dihydro-4oxyquinoline-3- carboxylate with boric acid in the presence of acetic anhydride and catalytic quantities of zinc to provide (1- cyclopropyl-6-fluoro-7-chloro-1,4 dihydro-4-oxyquinoline-3- carboxylate-O3, -O4) bis(acetateO) boron, subsequent treatment of the product with (1S, 4S)-5-methyl-2,5 diazabicyclo[2.2.1] heptane or an acid addition salt of the same, possibly in the presence of a base, to yield the intermediate (1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(1S,4S)-5- methyl-2,5-diazabicyclo [2.2.1] hept-2-yl-4-oxo-3-quinoline carboxylate-O3, -O4) bis (acetate-O) boron and finally hydrolysis to obtain the desired product in high yield and purity, which is isolated from the reaction medium by conventional processes.
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