Category: 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 is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

28 grams of ulifloxacin dissolved at room temperatureIn a 14 ml volume ratio of 5:1 acetic acid in acetonitrile,Dissolve and filter at 10CThen add 16ml of 10M hydrochloric acid to the filtrate.And stirred at 10 C for 4 hours to complete the reaction.After filtration, the precipitate was collected and washed with acetonitrile and dried under vacuum at 20C.The collected crystals were dissolved in methanol,After heating and stirring, cool in an ice bath and stir to crystallize.Precipitated crystals were collected and vacuum dried at 20C.That is, ulifloxacin hydrochloride crystal A is obtained.

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; Zhaoke Pharmaceutical (Hefei) Co., Ltd.; Li Xiaoyi; Dai Xiangrong; Zhou Guanqun; (18 pag.)CN107501298; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Synthesis of e-Ffuoro–methyl-T-l^ l-Cl-methyl-S-nitro-iniidazol- l-y)-ethyl]-piperazm-l -yl}-4-oxo-4H-2-th5a-8b-aza-cyclobiita[a]naphihafene- 3-carboxyfic acid (119): To a stirred solution of 6-Fluoro- l -methyl-4-oxo-7- piperazin- 1 -yl-4H-2-ihia-8 -aza-cyclobuta[a]naphihaiene-3-earboxyiic acid, (II) (5. 1 6g. 14,76 mmol ) in dimethylforrnarnide ( 1 00ml) was added potassium carbonate (2.03g, 14.76 mmol) followed by addition of compound (I) (2g, 7.2 mmol) and the reaction mixture was heated at 90 C for 16h. The reaction mixture was di luted with ethyl acetate, washed twice with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while eluting with 4-5% methanol/dichlorornethane mixture to obtain the pure compound ( 1 19) with 20% isolated yield. FontWeight=”Bold” FontSize=”10″ H-NMR (400 MHz, CDCI3) 5ppm: 2.12 (3H, d, J = 6.4 Hz, CH3), 2.52 (3H, s, CH3), 2.64 (4H, m, 2 xCH2), 2.72(2H, t, J = 6 Hz, CH2), 3.1 1 -3. 18 (4H, m, 2 x CH2), 4.43-4.49 (2H, m, CH2N). 5.8-5.9 ( 1 H, q, J,= 6.4Hz, J2 = 1 2.8Hz, CHSN), 6.3 (3 H, d, J = 6.8Hz, Ar- H), 7.92 (1 H, s, Ar-H), 7.95 ( 1 H, s, Ar-H). ESf-MS (m/z): 503 (M+H)

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

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

Example 2 Preparation of (R)-(+)-uliflourxacin; 105 g of racemic uliflourxacin was dissolved in 1,500 mL of DMSO. 27 g of L-tartaric acid was dissolved in 405 mL dimethyl sulfoxide dropwise while stirring to allow that the solution became turbid and the precipitation occurred. The solution was stirred at room temperature for 20 hours and then filtered. The collected solid was dried under vacuum to obtain 82 g solid which was recrystallized in dimethyl sulfoxide to obtain 34 g of dextrouliflourxacin-L-tartarte. Said salt was added into water to obtain a suspension, and the pH value was adjusted to 7-8 with 2% NaOH aqueous solution while stirring. After filtration and drying, 22 g of (R)-uliflourxacin was obtained, having a chemical name (R)-(+)-6-fluoro-1-methyl-4-oxo-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline -3-carboxylic acid. Specific rotation [alpha]20D= +132.4 (c=0.5, 0.1 mol/L methanesulfonic acid), optical purity e.e. 96%., 112984-60-8

As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; Hainan Hualon Pharmaceutical Co., Ltd.; EP2524922; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 DCC (0.9 g, 4.3 mmol)in DMF (20 ml), BOC-glycine (0.5 g, 2.85 mmol) and hydroxybenzotriazole (HOBt, 0.5 g, 4.3mmol) were added at 0 C and the mixture was allowed to stir for 4 h, followed by addition of 6-fluoro- 1 -methyl-7-(4-((5-nitro- 1H-benzo[d]imidazol-2-yl)methyl)piperazin- 1 -yl)-4-oxo- 1H,4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (0.9 g, 2.85 mmol) and triethylamine (0.4 g, 0.6 ml 4.3 mmol) at 0 C. The reaction mixture was allowed to stir for overnight at room temperature. After completion, the final solution was then concentrated under reduced pressure to obtain the crudeproduct which was purified by flash column chromatography over silica gel using 3% methanolDCM as eluent to afford compound A as pale yellow solid (0.75g, yield: 65%).1H NMR (DMSO-d6):oe 14.62 (brs, 1H, COOH), 7.84 (d, 1H, JAB = 14.0 Hz, ArH), 6.95 (d, 1H, JAB = 7.0 Hz, ArH), 6.81 (t, 1H, JAB = 6.0 Hz, NH), 6.39 (q, 1H, JAB = 6.5 Hz, SCHN), 3.85 (d, 2H, JAB = 6.0 Hz, CH2), 3.64-3.56 (m, 4H, CH2N), 2.12 (d, 3H, JAB = 6.0 Hz, CH3). ESI-MS (mlz): 495.16 (M+H).

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

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

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

Synthesis of 7-{4-[l~Chlowmethyi-2-(2-methyl-5-niiro mid zol-l-yl)- ethoxycarbonylmeihyl J-piperazin-1 -yl }-6~fl uoro- 1 ~methyl~4~oxo-4H~2~thia-8b~ aza-cyclobuia[a]naphthalene~3-carboxylic acid (1): To a stirred solution of 6- Fluoro- 1 -methy l-4-oxo-7-piperazin- 1 -y l~4H-2-thia~8b-aza~ cyclobuta[a]naphthalene-3-carboxylic acid, (III) (0.07 Ig, 0.2 mmol) in dimethylformamide (10ml) was added potassium carbonate (0.04g, 0.3 mmol) followed by addition of compound (II) (O.lg, 0.3 mmol) and the reaction mixture was stirred at RT for 3h. The reaction mixture was diluted with ethylacetate, washed two times with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while eluting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (1), i.e., Compound 90 from Table 1, with 30% isolated yield. H-NMR (400 MHz, DMSO) 6ppm: 2.19 (3H, d, J = 6.4 Hz, CH3), 2.57 (3H, s, CH3), 2.7 (4H, m, 2 x CH2), 3.1-3.3 (2H, s, COCH2), 3.32 (4H, m, 2 x CH2), 3.77-3.90(2H, ddd, Jx = 3.6 Hz, J2 = 12.4 Hz, J3 = 35.2 Hz, CH2C1), 4.40- 4.56 (1H, dd, Ji = 9.6 Hz, J2 = 14 Hz CHN), 4.76 (1H, d, J = 14 Hz, CHN), 5.44 (1H, d , J-5.6Hz CHOCO), 6.0-6.1 1 (1H, q, Jx = 6 Hz, J2 = 12.4 Hz, CHSN), , 6.4 (1H, d, Jx = 6.8 Hz Ar-H), 7.8 (1H, d, J = 14 Hz, Ar-H), 8.04 (1H, s, Ar-H). ESI-MS (m/z): 609 (M+H)+.

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

To a stirred solution of 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1H,4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (280 mg, 0.80 mmol) and triethylamine (0.3 ml , 2.16 mmol) in DMF(5 ml), compound C (570 mg, 1 mmol) was added and final solution was stuffed at room temperature for overnight. After completion, the solvent was evaporated, extracted with ethylacetate and washed with water. The organic extract was evaporated to obtain the crude mass which was further purified by flash column chromatography over silica gel using 2% methanol- DCM as eluent to obtain the compound D as an off white solid (220 mg, 48%). 1H NMR (DMSO-d6): 1H NMR (CDC13): isomer I: oe 14.66 (s,1H, COOH), 10.07 (s, 1H, NH), 8.66 (d, 1H, JAB= 1.5 Hz, ArH), 7.96 (s, 1H, ArH), 7.82 (d, 1H, JAB= 14.0 Hz, ArH), 7.70-7.66 (m, 1H, ArH), 6.95 (d, 1H, JAB= 7.0Hz, ArH), 6.40 (q, 1H, JAB = 6 Hz, SCHN), 3.44-3.37 (m, 4H, CH2N), 3.29 (s, 2H, CH2), 2.80-2.75(m, 4H, CH2N), 2.13 (d, 3H, JAB = 6.0 Hz, CH3), 1.64 (s, 9H, CH3), 1.36 (s, 18H, CH3); Isomer II: oe14.66 (s,1H, COOH), 10.01 (s, 1H, NH), 8.15 (d, 1H, JAB= 1.5 Hz, ArH), 7.90 (d, 1H, JAB= 9 Hz,ArH), 7.82 (d, 1H, JAB= 14.0 Hz, ArH), 7.70-7.66 (m, 1H, ArH), 7.51 (dd, 1H, JAB= 8.5 Hz, Jm= 1.5Hz,ArH), 6.95 (d, 1H, JAB= 7.0 Hz, ArH), 6.40 (q, 1H, JAB = 6 Hz, SCHN), 3.44-3.37 (m, 4H,CH2N), 3.29 (s, 2H, CH2), 2.80-2.75 (m, 4H, CH2N), 2.13 (d, 3H, JAB = 6.0 Hz, CH3), 1.64 (s, 9H,CH3), 1.36 (s, 18H, CH3)., 112984-60-8

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

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

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.

Synthesis of 6-Ffuoro-7-{4-[5-hydroxy-6-(2-methyl-5-nitro- imidazoi-I-yi)-hexyl]-piperazin-I-yi}-l -methyS-4-oxo-4H-2-thia-8b-aza- cyclobu a[a]naphthaSene-3-carboxylic acid (1 15): To a stin-ed solution of 6- Fluoro- 1 -methy-4-oxQ-7-piperazin- 1 -yl-4H-2-thia-8P-aza- cyclobuta[a]naphthalene-3-carboxylic acid, (HI) ( 1 .10 g, 3.16 mmol) in dimethylformamide (30ml) was added potassium carbonate (0.43g, 3.16 mmol) followed by addition of compound (II) (0.85g, 2.63 mmol) and the reaction 1 26 mixture was stirred at RT for 1 6h. The reaction mixture was diluted with ethyl acetate, washed twice with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while euting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (115) with 20% isolated yield. 1 H-NMR (400 MHz, DMSO) delta ppm: 1 .61 – 1 -68(6H, m, CH2), 2.1 (3H, d, J = 6 Hz, CH3), 2.44 (3H, s, CH3) , 2.54 (4H, m, 2 xCH2), 3.2 (4H, m, 2 xCH2), 3.9-4. 1 (2H. m, 2 x CH2N), 4.38( 1 H, d, J = 14, CHOH). 5.2 1 1 H, d, J = 4.4, OH), 6.38 ( 1 H, d, J = 5.6Hz, CHSN) 6.9 ( 1 H, d, J = 6.8, Ar-H). 7.78 ( 1 H, d, J = 1 4 Hz, Ar-H). 8.02 ( 1 H, s, Ar-H). ESI-MS (m/z): 575(M+H)

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

Example 1 Preparation of (S)-(-)-uliflourxacin; 105 g of racemic uliflourxacin was dissolved in 1,500 mL of dimethyl sulfoxide. 27 g of D-tartaric acid was dissolved in 405 mL of dimethyl sulfoxide dropwise while stirring. After stirring at room temperature for 20 hours, the precipitate was filtrated. The collected solid was dried under vacuum to obtain 86 g solid, which was recrystallized in dimethyl sulfoxide to obtain 37 g of levoulifloxacin-D-tartrate, with C49.08%, H5.06%, N9.50%, S7.44% shown by elemental analysis (molecular formula: C16H16FN3O3S·1/2C4H6O6·H2O, calculated values: C48.86%, H4.78, N9.50%, S7.25%). Said salt was added into water to obtain a suspension, and the pH value was adjusted to 7-8 with 2% NaOH aqueous solution while stirring. After precipitation, filtration, and drying, 24.5 g of (S)-uliflourxacin was obtained, having a chemical name (S)-(-)-6-fluoro-1-methyl-4-oxo-(1-piperazinyl)-1H,4H-[1,3]thiazeto [3,2-alpha]quinoline-3-carboxylic acid. Specific rotation [alpha]20D= -133 (c=0.5, 0.1 mol/L methanesulfonic acid); 1H-NMR (DMSO-d6) delta2.11 (3H, d, j=6.2 Hz), 2.87 (4H, m), 3.19 (4H, m), 6.40 (1H, q, j=6.2 Hz), 6.89 (1H, d, j=7.4Hz), 7.79 (1H, d, j=13.9Hz), optical purity e.e. 96%.

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; Hainan Hualon Pharmaceutical Co., Ltd.; EP2524922; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

Example 1 Preparation of (S)-(-)-uliflourxacin; 105 g of racemic uliflourxacin was dissolved in 1,500 mL of dimethyl sulfoxide. 27 g of D-tartaric acid was dissolved in 405 mL of dimethyl sulfoxide dropwise while stirring. After stirring at room temperature for 20 hours, the precipitate was filtrated. The collected solid was dried under vacuum to obtain 86 g solid, which was recrystallized in dimethyl sulfoxide to obtain 37 g of levoulifloxacin-D-tartrate, with C49.08%, H5.06%, N9.50%, S7.44% shown by elemental analysis (molecular formula: C16H16FN3O3S·1/2C4H6O6·H2O, calculated values: C48.86%, H4.78, N9.50%, S7.25%). Said salt was added into water to obtain a suspension, and the pH value was adjusted to 7-8 with 2% NaOH aqueous solution while stirring. After precipitation, filtration, and drying, 24.5 g of (S)-uliflourxacin was obtained, having a chemical name (S)-(-)-6-fluoro-1-methyl-4-oxo-(1-piperazinyl)-1H,4H-[1,3]thiazeto [3,2-alpha]quinoline-3-carboxylic acid. Specific rotation [alpha]20D= -133 (c=0.5, 0.1 mol/L methanesulfonic acid); 1H-NMR (DMSO-d6) delta2.11 (3H, d, j=6.2 Hz), 2.87 (4H, m), 3.19 (4H, m), 6.40 (1H, q, j=6.2 Hz), 6.89 (1H, d, j=7.4Hz), 7.79 (1H, d, j=13.9Hz), optical purity e.e. 96%.

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; Hainan Hualon Pharmaceutical Co., Ltd.; EP2524922; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

Acetonitrile (560 ml) and potassium bicarbonate (8 gm) are added to 6- fluoro-i-methyM-oxo-y-CI-piperazinyO^H-CI .SKhiazetofS^-alquinoline-S- carboxylic acid (14 gm, obtained as per the processes described in examples 1 and 2) under stirring at 25 – 300C, the contents are cooled to 150C and then the solution of 4-bromomethyl-5-methyl-1 ,3-dioxolen-2-one (10 gm) in acetonitrile (140 ml) is added at 15 – 200C for 30 to 45 minutes. The contents are stirred for 25 hours at 25 to 300C, filtered and the resulting filtrate is distilled under vacuum. To the residue added acetonitrile (70 ml), cooled the mass to 200C and then stirred for 1 hour to 1 hour 30 minutes at 20 – 250C. Filtered the solid, washed the solid with 15 ml of chilled acetonitrile and then dried to give 16 gm of prulifloxacin crude (HPLC Purity: 98.8%).To the prulifloxacin crude (obtained above) added acetonitrile (200 ml) at 25 – 300C, the contents are heated to reflux and then refluxed for 30 minutes. To the reaction mass added activated carbon (5 gm) and refluxed for 15 minutes. The reaction mass is filtered on hi-flo bed, the resulting filtrate is cooled to 200C and then stirred for 3 – 4 hours at 20 – 250C. Filtered the solid, washed with 20 ml of acetonitrile and then dried to give 14 gm of prulifloxacin (HPLC Purity: 99.9%)., 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; HETERO DRUGS LIMITED; WO2008/59512; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics