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

Some tips on 1,4-Di-Boc-piperazine-2-carboxylic acid

The synthetic route of 181955-79-3 has been constantly updated, and we look forward to future research findings.

181955-79-3, 1,4-Di-Boc-piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

181955-79-3, Step-2 [0552] Method-A [0553] (i) To a dichloromethane (DCM, 40 ml) solution of Boc-protected acid (5.0 g, 15.18 mmol) as prepared in step-1 is added a solution of N-hydroxysuccinimide (1.75 g, 15.21 mmol) in THF (20 ml) and a solution of DCC (3.6 g, 17.47 mmol) in DCM (20 ml) at 0 C. in the order specified. Reaction mixture stirred at 0-5 C. for 4-5 hrs, filtered, filtrate washed successively with water, aqueous sodium bicarbonate solution and finally with brine. Organic layer dried (Na2SO4) evaporated in vacuo to give the product as white solid. (Yield 5.8 g, 86.05%). [0554] (ii) To a solution of the succinimide derivative (1.92 g, 4.49 mmol) in DCM (20 ml) as prepared in (i) of step-2, is added a solution of L-prolinamide (0.6 g, 5.26 mmol). Reaction mixture stirred at 25 C. for 16 hrs. washed with aqueous NaHCO3 solution and brine, dried (Na2SO4), evaporated in vacuo yielding a crude residue. Desired coupled product was isolated by column chromatography (40% ethyl acetate/hexane), (Yield 0.53 g, 27.74%).

The synthetic route of 181955-79-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TORRENT PHARMACEUTICALS LTD.; US2004/106802; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 162046-66-4

As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

162046-66-4, (3-Pyrrolidin-l-ylphenyl)methylamine (8 g; 0.0408 mol) was dissolved in DCM (50 ml). Et3N (25 ml; 0.178 mol) was added to a stirring solution. l-(l,l-dimethylethyl)-4- (4-carboxyphenyl)-l-piperazinecarboxylic acid ester (10.429 g; 0.034 mol) was added and the mixture was stirred. CH2Cl2 (100 ml) was added and then DECP (11.9 ml; 0.0796 mol) was added. The reaction mixture was stirred for 18 hours. Then the mixture was stirred in a saturated NaHCO3-solution. The organic layer was separated, dried with MgSO4, filtered off, evaporated and co-evaporated with toluene. Yield : 15.815 g of intermediate 51 (99 %).

As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/148868; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of (R)-4-Benzyl 1-Boc-2-methylpiperazine-4-carboxylate

Big data shows that 128102-16-9 is playing an increasingly important role.

128102-16-9, (R)-4-Benzyl 1-Boc-2-methylpiperazine-4-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1 15Btert-Butyl 2-methylpiperazine- 1 -carboxylate[00728] A solution of 4-benzyl 1-tert-butyl 2-methylpiperazine- 1,4-dicarboxylate (4.8 g, 14.4 mmol) in methanol (25 mL) was added 480 mg of 10% Pd/C and stirred at room temperature under hydrogen overnight. Filtered and concentrated to give the title product (2.8 g, yield 97%) as colorless oil. ^-NMR (400 MHz, CDC13) delta (ppm): 1.21 (d, J= 6.8 Hz, 3H), 1.46 (s, 9H), 2.64-2.70 (m, 1H), 2.74- 2.78 (m, 1H), 2.88-3.01 (m, 3H), 3.78 (d, J= 12.4 Hz, 1H), 4.16 (m, 1H); LC-MS (ESI) m/z: 201 (M+l)+., 128102-16-9

Big data shows that 128102-16-9 is playing an increasingly important role.

Reference£º
Patent; BIOMARIN PHARMACEUTICAL INC.; WANG, Bing; CHU, Daniel; WO2011/130661; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 162046-66-4

As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example Al 6; a) Preparation of intermediate 43; A mixture of intermediate 11 (0.918 g; 3 mmol), EDCI (0.843g; 4.4 mmol), HOBt (0.594 g; 4.4 mmol) and 10 ml of DMF was stirred at room temperature for 15 minutes. Phenylacetic acid hydrazide (1 g; 6.65 mmol) was added. The mixture was stirred at room temperature for 18 hours. The solvent was evaporated. The residue was stirred in water and extracted with CH2Cl2. The organic layer was dried, filtered and evaporated. The residue was purified by reversed-phase high-performance liquid chromatography (Shandon Hyperprep C 18 BDS (Base Deactivated Silica) 8 mum, 250 g, LD. 5 cm). A gradient with the following mobile phases was applied. Phase A: a 0.25 % NH4HCO3 solution in water; phase B (optional): CH3OH; phase C: CH3CN). The desired fractions were collected and the solvent was evaporated. The residue was dried, yielding 0.802 g of intermediate 43., 162046-66-4

As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/148840; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid

The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

b) Preparation of intermediate 12; A mixture of intermediate 11 (6.7 g, 0.0220 mol), N’-(ethylcarbonimidoyl)-iV,jV- dimethyl-l,3-propanediamine, monohydrochloride (4.79 g, 0.0250 mol), 1-hydroxy- lH-benzotriazole (3.38 g, 0.0250 mol) and DMF was stirred at room temperature for 30 minutes. Neta3 was passed through the solution for 5 minutes (cooling with ice) and the mixture was stirred at room temperature for 18 hours. NH3 was passed again for 5 minutes through the solution and the mixture was stirred for 2 hours at room temperature. H2O (50 ml) was added and the product was precipitated. The product was filtered off, washed with water and dried, yielding 5.77 g (85 %) of intermediate 12., 162046-66-4

The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/148840; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate

113028-17-4 Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate 10249018, apiperazines compound, is more and more widely used in various fields.

113028-17-4, Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,113028-17-4

Example 10: Preparation of prulifloxacin hydrochloride; Method A: To the mixture of dimethylformamide (1.5 It) and 6-fluoro-l-methyl-4-oxo-7-(l- piperazinyl)-lH,4H-[l,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (0.3kg), 4-bromomethyl-5- methyl- 1, 3 -dioxolen-2-one, obtained above was added and cooled to 0-50C. Triethylamine (0.87kg) in dimethylformamide (0.3 It) was added slowly in 1-2 hours. After completion of the reaction (monitored by TLC), dichloromethane (3.0 It) and water (1.5 It) were added to the reaction mixture. The layers were separated and aqueous layer was extracted twice with dichloromethane (1.5 It). All organic layers were combined, dried over sodium sulfate followed by distillation. Methanolic hydrochloride (20-25 % w/w, 0.24 It) was added to organic layer at 0- 5C and stirred. The solid, thus precipitated out was filtered, washed with dichloromethane and dried to obtain 0.36kg of the title compound having purity 92.73 % by HPLC. Example 11: Purification of prulifloxacin hydrochlorideDimethylformamide (1.34 It) was added to prulifloxacin hydrochloride (67g) and reaction mass was heated to 110-112C for 1 hour. The reaction mixture was cooled to 25-300C and stirred for 2 hours, filtered, washed with N,iV-dimethylforamide. The product was slurry washed with isopropanol (0.670 It) and dried to obtain 48.8g of title compound having purity 99.30 % by HPLC.

113028-17-4 Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate 10249018, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; IND-SWIFT LABORATORIES LIMITED; WO2009/93268; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

At room temperature, 20 g of yufloxacin and 400 ml of a 18% methanol solution of hydrogen chloride (i.e., methanolic hydrochloric acid) were added to a 1000 ml Erlenmeyer flask, and the material was rapidly dissolved by stirring at room temperature for 10 minutes. The resulting solution was colorless and transparent, the reaction was continued stirring for 30 minutes, filtered, and the precipitated crystals were collected. The resulting crystals were collected under vacuum at 20C. The resulting crystals were collected in the proportion of 1g: 2ml water was dissolved in water and heated to dissolve, filtered, the filtrate was collected and allowed to cool to room temperature, the filtrate was added 1 volume filtrate of acetone, stirred precipitation, the precipitation of crystals collected in 20 C under vacuum drying, the sample gradually turned white to pale yellow solid, that is the present invention is water-soluble, The obtained compounds were characterized by X-ray powder diffractometry, differential scanning calorimetry, nuclear magnetic resonance, and infrared spectroscopy, respectively, and their characterization spectra were shown in FIG. 1 to FIG. 6 as crystal B. FIG., 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; Zhaoke Pharmaceutical (Hefei) Co., Ltd.; Li Xiaoyi; Dai Xiangrong; Zhou Guanqun; (20 pag.)CN107383069; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 162046-66-4

162046-66-4, The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

4- (4- (tert-Butoxycarbonyl) pirhoerazin-1-yl) benzoic acid (10 g, 32.64 mmol) was dissolved in anhydrous THF (200 mL) under nitrogen at O0C and BH3. THF (IM in THF, 65.3 mL, 65.3 mmol) was added over 15 min. The reaction was EPO maintained at this temperature and after 3 h a further portion of BH3-THF (IM in THF, 10 mL, 10 itimol) was added. After 2 h, MeOH (30 mL) was added and the reaction was warmed to rt. The reaction mixture was partitioned between EtOAc (150 mL) and brine (200 mL) . The aqueous layer was re-extracted with EtOAc (100 ruL) and the combined organics were washed with a saturated aqueous solution of NaHCXb (150 mL) and then dried (MgSO/j) and filtered. On concentration of the solution the title compound (8.57 g, 90%) precipitated as a white solid and was collected by filtration. 1H NMR (CDCl3) 1.51 (9H, s), 8.14 (4H, t) , 3.62 (4H, t) , 4.62 (2H, d) , 6.94 (2H, d) , 7.31 (2H, d) .

162046-66-4, The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2007/27528; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics