Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step B: tert-butyl(9aS)-3-hydroxy-3-( 1 -oxo-3.4-dihydro- 1H-isochromen-6- yl)hexahydropyrazino [2,1-c] [1,41 oxazine-8( 1H)-carboxylate: 6- (Bromoacetyl)-3 ,4-dihydro- 1H- isochromen-1-one (-.1.54 g, -.5.72 mmol, presence of cx-chloroketone was noted, -.10%) and commercially available (S)-4-N-BOC-2-hydroxymethylpiperazine (1.24 g, 5.72 mmol) were added to a round bottom flask and diluted with THF (50 mL). Diisopropylethylamine (1.30 mL,7.44 mmol) was then introduced and the mixture left stirring for 14 h at RT during which time a considerable amount of solid had formed. The reaction mixture was diluted with EtOAc, then washed with saturated NH4C1aq followed by H20. Both aqueous layers were sequentially back extracted once with another portion of EtOAc, the organics were then combined, dried with MgSO4, filtered, and concentrated in vacuo. The recovered crude product was subjected topurification by flash chromatography (Biotage, 50% EtOAc/Hex) to afford the title compound

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
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694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

After taking the two 50mL round bottom flask was added sequentially aniline compound 5 (1.10mmol), NaNO2 (2.21mmol), ultrapure water (20 mL), the system was cooled to 0 deg.] C, was slowly added dropwise HCl (3.30mmol) in 5mL aqueous solution The After the addition, maintain the temperature of the reaction system continue to react 1.5h. It was then slowly added dropwise an aqueous solution of NaN3 (1.32mmol). After the addition was complete, maintainingThe reaction temperature of the reaction system, 3h, TLC monitored the reaction. After completion of the reaction, a saturated NaHCO3 solution was added 20mL, extracted with ethyl acetate 30mL ¡Á 2, combined organic phases were dried over anhydrous Na2SO4, and concentrated to give azide 6 directly administered next.

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Tianjin International Bio-pharmaceutical Joint Institute; Rao Zihe; Bai Cuigai; Yang Cheng; Chen Yue; Li Huiying; Wang Lei; Gao Yuan; Yang Juan; Sun Tao; Zhong Chuanke; (26 pag.)CN106749278; (2017); 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.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

A mixture of 4-((4-ethylpiperazin- 1 -yl)methyl)-3-(trifluoromethyl)aniline (Intermediate Cl)(500 g, 1.74 mmol) and methyl 3-hydroxybenzoate (Intermediate B2) (317 mg, 1.91 mmol)in anhydrous THF (5.0 mL) was cooled to -20 C and added potassium tert-butoxide (1M, 10 mL, 10.44 mmol). The mixture was stirred at RT for 3 h. The reaction mixture was cooled to-20 C and quenched with saturated sodium bicarbonate solution. The aqueous mixture was extracted twice with ethyl acetate and the combined organic layers were washed with waterfollowed by brine. The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated to yield 220 mg of the desired product. ?H NMR (400 MHz, DMSO-d6) oe 0.98 (t, J = 6.8 Hz, 3H), 2.31-2.50 (m, 8H), 2.51 (br s, 2H), 3.56 (s, 2H), 6.98-7.01 (br d, 1H), 7.3 1-7.35 (m, 2H), 7.39 (d, J = 6.4 Hz, 1H), 7.69 (d, J = 8.8 Hz, 1H), 8.03 (d, J = 8.4 Hz, 1H), 8.21 (s, 1H), 9.79 (s, 1H), 10.42 (s, 1H); ESI-MS (m/z) 408 (M+H).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference£º
Patent; GLENMARK PHARMACEUTICALS S.A.; PATEL, Vinod; REDDY, Venkateshwar; GHARAT, Laxmikant Atmaram; CHAUDHARI, Sachin Sundarlal; DAS, Sanjib; VELGALETI, Ranganadh; SHAH, Daisy Manish; BAJPAI, Malini; (262 pag.)WO2018/215668; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

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;,
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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%.

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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