8-Chloro-6,7-difluoro-1-[(1R,2S)-2-fluorocycloprop

Compound 3 (12.4 g, 34.3 mmol) was added in conc. hydrochloric acid (125 mL) and acetic acid (125 mL). The mixture was stirred at 120-130 °C for 2 h. After diluting with H2O (500 mL), the precipitate was filtered and washed with H2O and ether, dryness under reduce pressure to afford target 8-chloro-6, 7-difluoro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid compound with (1S, 2R)-1-fluoro-2-methylcyclopropane (8.72 g, 76.2 percent, compound 4) as a colourless solid.Compound 4 (8.2 g, 24.6 mmol) was dissolved in acetonitrile (25 mL), added (S)-N-[(oxoboryl)methylene]-5-azaspiro[2, 4]heptan-7-amine (8 g), at reflux for 5 h. The reaction mixture was cooled and filtered. Using acetonitrile-ethanol purified to give (S)-8-chloro-6-fluoro-4-oxo-7-(7-[{(oxoboryl)methylene}amino]-5-azaspiro[2, 4]heptan-5-yl0-1, 4-dihydroquinoline-3-carboxylicacid compound with (1S, 2R)-1-fluoro-2-methylcyclopropane( 8.7 g, 76.5 %, compounds 5).Compound 3 (12.4 g, 34.3 mmol) was added in conc. hydrochloric acid (125 mL) and acetic acid (125 mL). The mixture was stirred at 120-130 C for 2 h. After diluting with H2O (500 mL), the precipitate was filtered and washed with H2O and ether, dryness under reduce pressure to afford target 8-chloro-6, 7-difluoro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid compound with (1S, 2R)-1-fluoro-2-methylcyclopropane (8.72 g, 76.2 %, compound 4) as a colourless solid.II 100.0g, III 80.0g was dissolved in 2000 ml acetonitrile. Add 41.0g triethylamine. Raise the temperature to 80 C. After reacting 2h, TLC detection reaction finishes. Lowering the temperature to 0 C, after stirring 2h filtration, filtration cake 45 C hot air drying 6h yellow product obtained after IV 147.0g. Yield: 91.5%.EXAMPLE 7 (+)-8-Chloro-6-fluoro-1-[(1R, 2S)-2-fluorocyclopropyl]-7-[trans-2-oxa-5, 8-diazabicyclo[4.3.0]-nonan-8-yl]-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid STR20 A solution of 159 mg of 7-([S, S]-2-t-Butoxycarbonyl-2, 8-diazabicyclo[4.3.0]nonan-8-yl)-8-chloro-6-fluoro-1-[(1R, 2S)-2-fluorocyclopropyl]-1, 4-dihydro-4-oxoquinoline-3-carboxylic Acid In 20 ml of acetonitrile were dissolved 344 mg of EXAMPLE 6 8-Chloro-7-[3, 7-diazabicyclo[3.3.0]oct-1(5)-ene -3-yl]-6-fluoro-1-[(1R, 2S)-2-fluorocyclopropyl]-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid STR19 A solution of 318 mg of

Molecular Weight:317.65
XLogP3:3.4
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:2
Exact Mass:317.0066553
Monoisotopic Mass:317.0066553
Topological Polar Surface Area:57.6
Heavy Atom Count:21
Complexity:529
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes