Some tips on 112984-60-8

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.112984-60-8,6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid,as a common compound, the synthetic route is as follows.

6-Fluoro- 1 -methyl-4-oxo-7-(piperazin- 1 -yl)- 1 H,4H- [1,3 ]thiazeto[3 ,2-a] quinoline-3-carboxylic acid (3 g, 8.60 mmol) was suspended in DMF (50m1) under argon atmosphere and heated at 90 C. After obtaining a clear solution,triethylamine (2.4 ml , 17.10 mmol), compound A (2.12 g, 6.50 mmol) and tetrabutylammonium bromide (107 mg, 0.33 mmol) were added. Then the reaction mixture washeated for another 20 h at 90 C. After completion of the reaction, it was allowed to cool to room temperature and ethyl acetate was added into the reaction mixture. The obtained precipitate was filtered and filtrate was evaporated to dryness. The crude mass was re-dissolved in DCM and methanol and excess amount diethyl ether was added into this solution to obtain a brown mass which was purified by flash column chromatography over silica gel and pure compound 2 was elutedwith3% methanol-DCMmixture as a beige solid (250 mg) with 8% isolated yield. 1H NMR (CDC13):3 14.23 (brs, 1H, COOH), 7.92 (s, 1H, ArH), 7.89 (d, 1H, JAB = 12.0 Hz, ArH), 6.38 (d, 1H, JAB = 8Hz, ArH), 6.09 (q, 1H, JAB = 4 Hz,SCHN), 4.5 1-4.41 (m, 2H, NCH2), 3.26-3.20 (m, 4H, CH2N), 2.74(t, 2H, JAB = 4 Hz, NCH2), 2.69-2.67 (m, 4H, CH2N), 2.20 (d, 3H, JAB = 4 Hz, CH3). ESI-MS (mlz):503.20 (M+H)., 112984-60-8

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; GHOSH, Shamik; GHOSH, Sumana; SINHA, Mau; SADHASIVAM, Suresh; BHATTACHARYYA, Anamika; MAVUDURU, Siva Ganesh; TANDON, Nupur; KUMAR, Deepak; (149 pag.)WO2017/17631; (2017); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 6- fluoro- 1 -methyl-4-oxo-7-(piperazin- 1 -yl)- 1 H,4H- [1,3] thiazeto[3 ,2-a]quinoline-3-carboxylic acid (690 mg, 1.98 mmol) in DMF (10 ml), triethylamine (0.55 ml, 3.95 mmol) and compound B(500 mg, 1.97 mmol) were added and the reaction mixture was stirred at room temperature for 18 h. Aftercompletion of the reaction excess ethyl acetate was added into the reaction mixture and solids were filtered out. The crude obtained after concentrating the filtrate, was purified by flash column chromatography over silica gel using 8% methanol-DCM eluent to obtain 18 (135 mg, 13%) 1H NMR (DMSO-d6): oe 14.65 (brs, 1H, COOH), 13.09 (brs, 1H, NH), 8.47-8.35 (m, 1H, ArH), 8.12- 8.08 (m, 1H, ArH), 7.79 (d, 1H, JAB = 13.5 Hz, ArH), 7.65 (d, 1H, JAB = 8.5 Hz, ArH), 6.92 (d, 1H,JAB = 7.0 Hz, ArH), 6.37 (q, 1H, JAB = 5.5 Hz,SCHN), 3.91 (s, 2H, CH2), 2.76-2.62 (m, 4H, CH2N),2.01 (d, 3H, J = 6.0 Hz, CH3). ESI-MS (mlz): 525.07 (M+H)., 112984-60-8

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; GHOSH, Shamik; GHOSH, Sumana; SINHA, Mau; SADHASIVAM, Suresh; BHATTACHARYYA, Anamika; MAVUDURU, Siva Ganesh; TANDON, Nupur; KUMAR, Deepak; (149 pag.)WO2017/17631; (2017); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid

112984-60-8, The synthetic route of 112984-60-8 has been constantly updated, and we look forward to future research findings.

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Racemic ulifloxacin (105 g) was dissolved in DMSO (1500 mL). D-tartrate (27 g) solution in DMSO (405 mL) was added to the racemic ulifoxacin solution with agitation. Cloudiness and precipitation appear. After 20 hours of agitation at an ambient temperature, the mixture was filtered. The solid was dried under vacuum to yield 86 g of solid. The solid was recrystallized in DMSO to yield 37 g of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a] quinoline-3-carboxylic acid-D-tartrate salt; the elemental analysis indicates: C 49.08%, H 5.06%, N 9.50%, and S 7.44% (corresponding to: C16H16FN3O3S¡¤1/2C4H6O6¡¤H2O, calculated value: C 48.86%, H 4.78, N 9.50%, and S 7.25%). The salt was dispersed in water and the dispersion was neutralized witrh 2% NaOH aqueous solution to a pH value of 7 to 8. The precipitate is filtered and dried to yield 24.5 g of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeta[3,2-a]quinoline-3-carboxylic acid. It has a rotation [Show Image] (c = 0.15, 0.1 mol/L NaOH), 1H-NMR (DMSO-d6) delta2.11(3H, d, j=6.2 Hz), 2.85?3.20 (8H, m), 6.40(1H, q, j=6.2 Hz), 6.89(1H, d, j=7.4Hz), 7.79(1H, d, j=13.9 Hz), optical purity e.e.>95%.

112984-60-8, The synthetic route of 112984-60-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangzhou Baiyunshan Pharmaceutical Co. Ltd. Guangzhou Baiyunshan Pharmaceutica Factory; Guangzhou Pharmaceutical Industry Academe; EP2258705; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics