Month: August 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

Step 2: 5-Bromo-3-((2-(4-methylpiperazin-l- yl)ethylamino) methyl) pyridin-2-amineTriethylamine (1.0 mL, 7.09 mmol) was added to a solution of 2-amino-5- bromonicotinaidehyde hydrobromide (1.0 g, 3.54 mmol) in methanol (24 mL) at room temperature. The reaction mixture was stirred for 10 minutes prior to the addition of 2-(4-methylpiperazin-l-yl)ethanamine (558 mg, 3.90 mmol). The reaction mixture was then stirred overnight and cooled to 0¡ãC. Sodium borohydride (201 mg, 5.32 mmol) was added portionwise at 0¡ãC and the reaction mixture was allowed to reach room temperature and stirred for 4 hours. After concentration to dryness, the residue was purified by chromatography on silica gel using dichloromethane/methanol/ammoniac (10 : 0 : 0.1 to 9 : 1 : 0.1) as eluent. The title product was obtained as a yellow solid (560 mg, 48percent).LCMS (ESI-APCI) m/z 328.1-330.1 (M + H)+

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; FAB PHARMA SAS; GERUSZ, Vincent; ESCAICH, Sonia; OXOBY, Mayalen; DENIS, Alexis; WO2011/61214; (2011); 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.438631-77-7,(R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

1-tert-Butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (5.03 g, 20.59 mmol) was added to 670 7-bromo-4,6-dichloro-5-fluoro-3-nitroquinoline (3.5 g, 10.30 mmol) and 56 DIPEA (7.19 mL, 41.19 mmol) in 78 THF (50 mL) at rt. The resulting solution was stirred at 80 C. for 16 h. The solvent was removed in vacuo. The crude product obtained was purified by flash silica chromatography (0 to 20% 57 EtOAc in 148 petroleum ether) to afford 672 1-tert-butyl 3-methyl (3R)-4-(7-bromo-6-chloro-5-fluoro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (1.75 g, 31%) as a red solid; 1H NMR (300 MHz, DMSO, 30 C.) 1.45 (9H, s), 3.31 (3H, d), 3.37-3.45 (2H, m), 3.47-3.55 (2H, m), 3.68-3.82 (2H, m), 4.20-4.30 (1H, m), 8.45 (1H, d), 9.10 (1H, s); m/z: ES+ [M+H]+=547

438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Methanesulfonyl chloride (0.7 mL, 9.0 mmol) was added to a cooled solution of 4-(2-amino- ethyl)-piperazine-1-carboxylic acid tert-butyl ester (1.33 g, 5.8 mmol) in pyridine (25.0 mL). The reaction was stirred for 12 h and partitioned between partitioned between aqueous sodium bicarbonate and methylene chloride. The organic phase was washed with 1M hydrochloric acid, aqueous sodium bicarbonate, brine, dried over anhydrous magnesium sulfate and concentrated. Purification of the crude residue by chromatography over silica gel using 0-5percent methanol in methylene chloride gave 4-(2-methanesulfonylamino-ethyl)-piperazine-l- carboxylic acid tert-butyl ester (0.70 g, 70percent). To a cooled solution of 4-(2-methanesulfonylamino-ethyl)-piperazine- I -carboxylic acid tert- butyl ester (0.64 g, 0.2 mmol) in dioxane (20 mL) was added hydrochloric acid (4M in dioxane, 10 mL) and the reaction was stirred at room temperature for 12 h and concentrated to give N- (2-methanosulfonylethyl) -piperazine dihydrochloride as a white solid (0.55 g, 95percent).

192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; F.HOFFMANN-LA ROCHE AG; WO2005/110996; (2005); 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

CuCO3.Cu(OH)2.H2O (15.8 g) was added to the H2O (275 mL) solution of piperazine-2-carboxylic acid, dihydrochloride (22.3 g), then the mixture was refluxed and stirred for 10 min. The insoluble material was filtered off and was washed with hot H2O (165 mL). The filtrate was cooled to room temperature, and NaHCO3 (9.2 g) and 1,4-dioxane (220 mL) was added to the dark blue solution. The mixture was cooled to 0 C. and NaHCO3 (18.5 g) and 50% solution of 4-nitrobenzyl chloroformate in 1,4-dioxane (61.7 g) was added to the mixture for 0.5 h. After stirring for additional 1.5 h at 0 C., the precipitate was filtered and washed with cold H2O (140 mL), EtOH (100 mL), acetone (200 mL) and Et2O (100 mL), then it was allowed to dry under reduced pressure to obtain the pale blue crystals. The crystals were added to the 1 mol/L HCl (330 mL) solution of EDTA.2Na (20.5 g) for 30 min, and stirred for 2 h at room temperature. The suspension was filtered and the filtered material was diluted with EtOH-H2O (7:3, 550 mL) and refluxed for 10 min. The reaction mixture was filtered to obtain the colorless crystals. The recrystallization from the filtrate was carried out 3 times to obtain additional crystals. The combined crystals were dried under reduced pressure to obtain the titled compound (26.25 g, 77%) as colorless crystals. 1H NMR (D2O) delta 2.54-2.61 (m, 1H), 2.89 (dt, 2H, J=12.7, 3.4 Hz), 2.97 (br, 1H), 3.13 (br, 1H), 3.62-4.04 (m, 2H), 5.16 (s, 2H), 7.49 (d, 2H, J=8.6 Hz), 8.14 (d, 2H, J=8.6 Hz).

The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Wyeth; US2006/276445; (2006); 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.68104-63-2,4-(Piperazin-1-yl)benzonitrile,as a common compound, the synthetic route is as follows.

To t-butyl 4-(4-cyanophenyl)piperazine-1-carboxylate (2.30 g, 8.0 mmol, prepared by reaction of the aryl-piperazine with Boc-anhydride) in toluene (20 ml) add DIBAH (diisobutylaluminum hydride) (1.0M in toluene, 12.8 ml, 12.8 mmol). Heat at 50 C. 1.5 h, allow to cool, add MeOH (10 ml) and water (10 ml). Filter and concentrate. Chromatograph the residue over silica to obtain the Boc-piperazine as a yellow solid.

As the paragraph descriping shows that 68104-63-2 is playing an increasingly important role.

Reference£º
Patent; Schering Corporation; US2005/239795; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Example 8: Preparation of Ulifloxacin;Tertiary butanol (5.55It), 6-fluoro-l-methyl-4-oxo-7-(l-piperazinyl)-4H-[l,3]thiazeto [3,2- a]quinoline-3-carboxylic acid ethyl ester (1.1 lkg), potassium hydroxide (0.37kg) and water (2.75 It) were added at room temperature. The reaction mixture was heated to 600C and maintained for 1.5 hours. Reaction completion was checked by TLC. This was followed by the addition of water (22.2 It) and acetic acid (0.39 It). The reaction mixture was filtered, washed with water followed by slurry wash with acetone (2.22 It) twice and dried to obtain 0.95 kg of ulifloxacin having purity 97.56% by HPLC.

As the paragraph descriping shows that 113028-17-4 is playing an increasingly important role.

Reference£º
Patent; IND-SWIFT LABORATORIES LIMITED; WO2009/93268; (2009); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Compound bromo-2-fluoro-3-nitrobenzene 64a (3.1 g, 14.0 mmol), 1-tert-butoxycarbonyl (2S)-2-methylpiperazine(4.2 g, 21.0 mmol) and dioxane (50 mL) were mixed, and tris(bisbenzylideneacetone)palladium (0.6 g,0.7 mmol), 4,5-bisdiphenylphosphino-9,9-dimethyloxaxan (0.8 g, 1.4 mmol) and cesium carbonate (9.1 g, 28 mmol),The reaction was carried out under an argon atmosphere at 110 C for 16 hours. Cool to room temperature, extract with dichloromethane (100 mL¡Á3), and use organic phaseWash with saline solution (100 mL). Dry the organic phase with anhydrous sodium sulfate, remove the desiccant by filtration, and pass the residue through a flash column.Chromatography purification (petroleum ether / ethyl acetate = 5:1) afforded the desired product 1-t-butoxy acyl (2S)-4-(2-fluoro-3-nitrobenzene2-methylpiperazine 64b (2.6 g, 7.7 mmol, red oily liquid), yield: 55%.

#N/A

Reference£º
Patent; Nanjing Tianyinjianhua Pharmaceutical Technology Co., Ltd.; Kong Xianglong; Zhou Chao; Zheng Zhixiang; (105 pag.)CN109020957; (2018); A;,
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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

(6-Chloro-4,5-dimethyl-pyridazin-3-yl)-pyridin-2-yl-methanone (550 mg, 2.22 mmol), (R)-2-methyl-piperazine (320 mg, 3.20 mmol) are added into a microwave vial followed by NMP (6 mL) and triethylamine (0.92 mL, 6.66 mmol). The vial is sealed and irradiated in the microwave at 180¡ã C. for 1 h. The crude material is directly purified via flash chromatography on silica gel (20-70percent methanol in CH2Cl2) to afford the title compound (671 mg, 97percent). 1H NMR (400 MHz, DMSO-d6) delta=9.57 (br s, 1H), 8.66 (d, J=5.0 Hz, 1H), 8.10-8.17 (m, 2H), 7.69-7.73 (m, 1H), 3.65 (m, 1H), 3.62 (m, 1H), 3.45-3.50 (m, 1H), 3.12-3.33 (m, 4H), 2.29 (s, 3H), 2.15 (s, 3H), 1.32 (d, J=6.5 Hz, 3H).

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Novartis AG; US2010/41663; (2010); 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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of piperazine-1, 2-dicarboxylic acid 1-teit-butyl ester2-methyl ester (977 mg, 4.0 mmol) in DCM (20 mL) at 0 00 was added4-bromo-benzenesulfonyl chloride (1.02 mg, 4.0 mmol). Then TEA (404 mg, 4.0mmol) was added dropwise and the mixture was stirred at room temperature for 1hr. The mixture was concentrated and purified by silica gel chromatography(petroleum ether/EtOAc = 20/1 to 5/1) to afford 1.66 g (90%) of the titlecompound as a white solid. 1H NMR (400 MHz, ODd3) O [ppm] 7.69 (d, J = 8.8Hz, 2H), 7.61 (d, J= 8.8 Hz, 2H), 4.89-4.60 (m, 1H), 4.27-4.20 (m, 1H), 4.04-3.82(m, 1H), 3.77 (5, 3H), 3.76-3.61 (m, 1H), 3.35-3.11 (m, 1H), 2.51 (dd, J= 11.6, 4.0Hz, 1H), 2.33 (td, J= 11.6, 4.0 Hz, 1H), 1.44 (5, 9H).

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER INC.; ITEOS THERAPEUTICS; NINKOVIC, Sacha; CROSIGNANI, Stefano; SCALES, Stephanie Anne; MCALPINE, Indrawan James; COLLINS, Michael Raymond; MADERNA, Andreas; WYTHES, Martin; (295 pag.)WO2016/147144; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

STEP B: 2-ethyl-N-(3-fluoro-4-piperazin-1-yl-phenyl)-butyramide.To 4-(2-fluoro-4-methylamino-phenyl)-piperazine-1 -carboxylic acid tert- butyl ester prepared as in STEP A above and TEA (10.0 mmol) in CH2CI2 (50 mL) was added 2-ethyl-butyryl chloride (10.0 mmol). The resulting mixture was stirred at room temperature for 16 h. H2O (10 mL) was then added, the organic layer was separated. After concentration, the semi-solid was collected and re- dissolved into CF3COOH/CH2CI2 (10/50 mL). The resulting mixture was stirred at room temperature for 16 h, then concentrated to yield the title compound.

The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics