Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.,5271-27-2

General procedure: A mixture of 3 (2.91 g, 10 mmol), 4 (1.76 g, 10 mmol)and KF (18 mmol) were heated at 120-130 ¡ãC in DMF (30mL) for 16 – 18 h. At the end of this period, the reactionmixture was cooled to room temperature and diluted withwater (30 mL). The separated solid was filtered, washed anddried to obtain crude 6a-i. The obtained crude product wasthen purified by recrystallization using ethanol.

As the paragraph descriping shows that 5271-27-2 is playing an increasingly important role.

Reference£º
Article; Darsi, S.S. Praveen Kumar; Kumar, K. Shiva; Devi, B. Rama; Naidu; Dubey; Letters in Organic Chemistry; vol. 11; 8; (2014); p. 551 – 555;,
Piperazine – Wikipedia
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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.

Example 163 4-[4-(3-tert-Butyl-phenylcarbamoyl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester A mixture of 3-tert-butyl aniline (117 mg, 0.78 mmol), 4-(4-carboxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (prepared as described in ) (200 mg, 0.65 mmol), EDCI (375 mg, 0.95 mmol) and a catalytic amount of DMAP in CH2Cl2 was stirred at room temperature overnight. The next day the mixture was partitioned between EtOAc and water. The organic layer was collected, dried over Na2SO4, filtered and concentrated. The residue was chromatographed with silica gel column amd 0-30% EtOAc in hexanes gradient to afford the product (100 mg, Yield: 35%). HRMS m/z calcd for C26H35N3O3 [M+H]+: 438.2751; Found: 438.2753., 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; Madrigal Pharmaceuticals, Inc.; BOLIN, David, R.; CHEUNG, Adrian, Wai-hing; HAMILTON, Matthew, Michael; MARCOPULOUS, Nicholas; McDERMOTT, Lee, Apostle; QIAN, Yimin; EP2350311; (2013); B1;,
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74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (S)-2-methylpiperazine (1 g, 10 mmol, 1 eq) in DCM (30 mL) was added Trityl-CI (2.78 g, 10 mmol, 1 eq) portionwise at RT, then the reaction mixture was continued for 2 h. TLC analysis indicated formation of a less polar spot. The reaction mixture was quenched with water and extracted with EtOAc (3×50 mL). The combined organic layer was dried over Na2S04 then concentrated to give (S)-3-methyl-1-tritylpiperazine (3.3 g, 96%) as a colorless oil., 74879-18-8

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference£º
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ISAAC, Methvin; CHAU, Anh My; MAMAI, Ahmed; WATSON, Iain; PODA, Gennady; SUBRAMANIAN, Pandiaraju; WILSON, Brian; UEHLING, David; (191 pag.)WO2019/119145; (2019); 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.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

1-[4-(4-Amino-3-methyl-5-nitro-phenyl)-piperazin-1-yl]-ethanone: A mixture of 4-bromo-2-methyl-6-nitro-phenylamine (5 g, 21.64 mmol), 1-acetylpiperazine (4.2 g, 32.46 mmol), palladium acetate (244 mg, 1.08 mmol), tri-tert-butylphosphine (440 mg, 2.16 mmol) and sodium tert-butoxide (4.2 g, 43.29 mmol) in toluene (70 mL) was heated to 100 C. for 14 h under nitrogen. The reaction mixture was cooled to room temperature and diluted with EtOAc. After extraction, the combined organic layers were washed with water, brine, dried over Na2SO4. Concentration gave a brownish residue which was purified by flash column chromatography (10% MeOH/CH2Cl2) to yield the title compound (4.21 g, 70%). 1H NMR (400 MHz, CD3OD) delta 7.42 (1H, d, J=2.8 Hz), 7.23 (1H, d, J=2.8 Hz), 3.71 (2H, t, J=5.1 Hz), 3.67 (2H, t, J=5.1 Hz), 3.04 (2H, t, J=5.2 Hz), 2.98 (2H, t, J=5.2 Hz), 2.24 (3H, s), 2.31 (3H, s). LCMS (M+H)+m/z 279 (t=1.46 min.)., 13889-98-0

The synthetic route of 13889-98-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Beaulieu, Francis; Marinier, Anne; Ouellet, Carl; Roy, Stephan; Wittman, Mark D.; US2005/54655; (2005); A1;,
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76003-29-7,76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 4-Benzyl-3-oxo-piperazine-1-carboxylic acid tert-butyl ester Sodium hydride (60%, 18.11 g, 452 mmol) in mineral oil was triturated with 35 hexanes, dried under a stream of nitrogen and taken up in 1500 mL of THF. To the slurry at 0 C. was added 3-oxo-piperazine-1-carboxylic acid tert-butyl ester (75.057 g, 200.4 mmol) in portions over 15 min. After 90 minutes benzyl bromide (71.01 g, 415.1 mmol) was added and the mixture was warmed to room temperature for 18 hours. The solution was quenched with H2O and extracted with Et2O. The combined organic layers were washed with H2O, washed with brine, dried over MgSO4. Concentration in vacuo gave a crude solid which was recrystallized from hexane to afford 4-benzyl-3-oxo-piperazine-1-carboxylic acid tert-butyl ester (83.5 g, 76%) as a white crystalline solid.

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Roche Palo Alto LLC; US2009/209553; (2009); A1;,
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5464-12-0,5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1- (2-Hydroxyethyl) -4-methylpiperazine (199 mg, 1.38 mmol) , dicyclohexylcarbodiimide (310 mg, 1.50 mmol) and 4-dimethylaminopyridine (168 mg, 1.38 mmol) were added to a DMF solution (10 ml) of 3- [5-fluoro-3- (4- methoxyphenyl) -4-oxo-8-propoxy-4H-quinolin-l-yl] propionic acid (500 mg, 1.25 piunol) and stirred overnight at room temperature. Water was added to the reaction mixture, the mixture was extracted with dichloromethane and washed with water and then dried over anhydrous sodium sulfate. The dried product was concentrated under reduced pressure, and the resulting residue was purified using silica gel column chromatography (ethyl acetate –> dichloromethane : methanol = 10 : 1) . The residue was dissolved in ethyl acetate and a 4N hydrogen chloride ethylacetate solution was added thereto and stirred. The mixture was concentrated to dryness under reduced pressure, giving a pale yellow powder of 2-(4-methyl piperazin-1-yl) ethyl 3- [5-fluoro-3- (4-methoxyphenyl) -4-oxo-8-propoxy-4H-quinolin~ 1-yl] propionate dihydrochloride (110 mg, yield: 17percent) . Melting point: 150-1520C1H-NMR (DMSOd6) deltappm: 0.99-1.05 (3H, t, J=7.4 Hz), 1.69- 1.88 (2H, m) , 2.78 (3H, s) , 2.87-3.04 (2H, m) , 3.10-3.60 (1OH, m) , 3.77 (3H, s) , 4.01-4.11 (2H, t, J=6.8 Hz), 4.27- 4.44 (2H, m) , 4.67-4.94 (2H, m) , 6.76-7.09 (3H, m) , 7.16- 7.33 (IH, m) , 7.58-7.63 (2H, d, J=8.8 Hz), 8.07 (IH, s) .

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; OTSUKA PHARMACEUTICAL CO., LTD.; OTSUBO, Kenji; YAMAUCHI, Takahito; OCHI, Yuji; WO2010/64735; (2010); A1;,
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129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,129779-30-2

To a stirred solution of compound 1(2.1 g, 1 eq.) and compound 2 (2.3 g, 1 eq.) in ACN (20 mL), potassium carbonate (4.1 g, 3 eq.) was added. The reaction mixture was stirred at room temperature for 16 h. The reaction completion was monitored by TLC. The reaction mixture was diluted with water and extracted with ethyl acetate. The combined organic extracts were washed with water and brine, dried over anhydrous Na2504, filtered and concentrated under reduced pressure to give a crude residue which was purified by silica gel column chromatography to afford compound 3.

The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOMARIN PHARMACEUTICALS INC.; LUEDTKE, Gregory; BHAGWAT, Shripad; (99 pag.)WO2018/119362; (2018); A2;,
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5747-48-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11- piperazinyldibenzo[b,f] [l,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25- 30C, and, to which, was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 moles)] and 2-(2-chloroethoxy)ethanol [32.0 gm (0.257 moles)] at room temperature. The reaction mixture was heated to reflux at 110- 112C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check absence of compound of formula IV) and was cooled to 25C to 30C. To which, was added 150 cc DM water. Then the reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extracts and the organic layer were combined, and the pH was adjusted to 2-3 using IN HCl solution in DM (demineralized) water, the reaction mixture was then stirred for 30 min at 25-30C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH was adjusted to 8-10 using sodium carbonate, the reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extracted with 125 cc toluene. The extracts and the organic layer were combined, and washed with DM (demineralized) water 300 cc twice. The organic layer was distilled – off under vacuum below 70C to afford 2-(2-(4-dibenzo[b,f]-[l,4] thiazepine- l l-yl-l-piperazinyl)ethoxy)ethanol Purity of 2-(2-(4-dibenzo[b,f]-[l,4] thiazepine- l l-yl-l-piperazinyl)ethoxy)ethanol was 99.0 (area % by HPLC).

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/121415; (2008); 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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

4-({6-[ 1 -(tert-Butoxycarbonyl)- 1 H-indol-2-yl]pyrazin-2-yl}amino)-3- methoxybenzoic acid (20.0 mg, 0.04 mmol), l-(2-methoxyethyl)piperazine (10.4 mg, 0.07 mmol), TBTU (18.1 mg, 0.06 mmol) and TEA (7.5 muL, 0.06 mmol) in DMF ( 1 mL) were shaken at ambient temperature for 48h after which the temperature was raised to 1400C for 6h, let to ambient temperature and purified using preparative HPLC system A followed by system E. Yield 0.4 mg (2%). HPLC 100%, RT: 1.854 (10-97% MeCN over 3min). MS 487 (M+H)+., 13484-40-7

The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOVITRUM AB (PUBL); WO2007/147874; (2007); 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.1214196-85-6,1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

A 50 mL rb flask equipped with an air condenser, rubber septum and a magnetic stir bar was set under Ar atmosphere and charged with 500 mg of 1 -(/tv7-b utoxy carbonyl)piperazine-2- carboxylic acid (2.17 mmol, 1 equiv.), 80.0 mg of DMAP (0.651 mmol, 0.3 equiv.), 500 mg of EDCI (2.61 mmol, 1.2 equiv.), 10 mL of CH2CI2 and 3 mL of dry methanol. The reaction mixture was stirred at 40 C for 1.5 h and then the reaction was allowed to cool to rt. After stirring for 20 h, the reaction mixture was concentrated and the residue was dissolved in CH2CI2. The CH2CI2 solution was washed with water (3x). The water solutions were combined and the product was back-extracted with CH2CI2 (3x). Then the combined organics were washed with sat. NaHC03 solution, brine and dried over Na2S04. The crude product (661 mg) was purified on silica gel column using 0 to 5 % MeOH in CH2CI2 as eluent affording 419 mg (79 %) of the product 41 as a colorless oil.

1214196-85-6, The synthetic route of 1214196-85-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; ALTAS TAHIROVIC, Yesim; WILSON, Lawrence; PELLY, Stephen Christopher; (102 pag.)WO2019/183133; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics