Month: April 2021

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 81 2- [3 – (4- Acetyl-piperazin- 1 -yl) -phenyl] -6-chloro-3 ,3 -dimethyl- 1 ,2,3 ,4-tetrahydro- quinoline-8-carboxylic acidTo a mixture of 2-(3-bromo-phenyl)-6-chloro-3,3-dimethyl-l,2,3,4-tetrahydro-quinoline- 8-carboxylic acid methyl ester (410 mg, 1 mmol), palladium acetate (6.73 mg, 0.03 mmol), cesium carbonate (0.65 g, 2 mmol), xantphos (23 mg, 0.04 mmol) and N-acetylpiperazine (192 mg, 1.5 mmol) in toluene (10 mL) was stirred at 120C for 12 hours. Then the reaction mixture was concentrated in vacuo and the residue was extracted with ethyl acetate (2 x 100 mL), washed with saturated aqueous sodium chloride (2 x 50 mL), dried over anhydrous sodium sulfate and concentrated in vacuo. Purification on flash silica gel chromatography (silica gel from QingDao, 200-300 mesh, glass column from Shanghai SD company)(20% ethyl acetate/hexanes) to afford 2- [3-(4-acetyl-piperazin-l-yl)-phenyl] -6- chloro-3,3-dimethyl-l,2,3,4-tetrahydro-quinoline-8-carboxylic acid methyl ester (0.25 g, 54%) as a white solid: LC/MS m/e calcd for C25H30CIN3O3 M+: 455.99, observed: 456.1., 13889-98-0

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; CHEN, Li; FENG, Lichun; HUANG, Mengwei; LIU, Yongfu; WU, Guolong; WU, Jim, Zhen; ZHOU, Mingwei; WO2011/128251; (2011); A1;,
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109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 5 (Synthesis of 4-[(4-methyl-1-piperazinyl)methyl]benzoic acid 4-(Chloromethyl)benzoic acid (58 g) is added to a solution of N-methylpiperazine (150 g) in n-BuOH (580 g) at room temperature. After stirring for 3-6 h, the solvent is evaporated under reduced pressure and the residue is taken up with IPA (440 g). The mixture is refluxed for 15 min under stirring, then stirred for 24 h at room temperature. The solid is filtered off, washed with IPA (2*58 g) and dried under vacuum at 70 C. overnight. The desired product is obtained as a white solid (59.5 g, 75% yield).

109-01-3, As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Patent; MacDonald, Peter; Rossetto, Pierluigi; US2008/103305; (2008); A1;,
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Piperazines – an overview | ScienceDirect Topics

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,75336-86-6

(R)-2-methylpiperazine (5.025 g, 50.2 mmol) was dissolved in DCM (100 mL). A solution of boc anhydride (5.47 g, 25.1 mmol) in DCM (50 mL) was added dropwise at 0 C. The reaction mixture was stirred at rt for 1 h. The solution was filtered and concentrated under reduced pressure. H2O (100 mL) was added to the residue, which was filtered again. The filtrate was saturated with K2CO3 and extracted with Et2O (3*150 mL). The combined organic layers were dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure to provide 5.04 g Intermediate D (50%) as a solid. 1H NMR (300 MHz, CDCl3) delta ppm 1.03 (d, J=6.3 Hz, 3H) 1.45 (s, 9H) 1.56 (s, 1H) 2.30-2.46 (m, 1H) 2.65-2.72 (m, 1H) 2.74-2.76 (m, 2H) 2.93-2.95 (m, 1H) 3.93 (br s, 2H). Intermediate D is also commercially available from Lanzhou Boc Chemical Co.

75336-86-6 (R)-2-Methylpiperazine 7330434, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; COLLINS, Craig D.; US2011/201622; (2011); A1;,
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5521-38-0, 2-(4-(4-Nitrophenyl)piperazin-1-yl)ethanol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5521-38-0

Step: 3A-2Synthesis of 2-[4-(4-Amino-phenyl)-piperazin-l-yl]-ethanol.Procedure:Pd-C (0.3g) was added to a solution of 2-[4-(4-Nitro-phenyl)-piperazin-l-yl]-ethanol (3g, 0.01195mol) in MeOH (20ml) and hydrogenated for 2hrs. The reaction was monitored by the TLC (20% MeOH: CHC13). The resultant was filtered, washed with MeOH and concentrated to afford 1.8g (69% yield) of 2-[4-(4-Amino-phenyl)-piperazin-l-yl]-ethanol as a pink solid.

As the paragraph descriping shows that 5521-38-0 is playing an increasingly important role.

Reference£º
Patent; AURIGENE DISCOVERY TECHNOLOGIES LIMITED; SENGUPTA, Saumitra; RAJAGOPALAN, Srinivasan; BELAVAGI, Ningaraddi; RAMACHANDRA, Muralidhara; WO2012/59932; (2012); A1;,
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5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5625-67-2, Step 1 tert-butyl 4-benzyl-3-oxopiperazine-1-carboxylate Di-tert-butyl dicarbonate (750 mg, 3.44 mmol) was added to a solution of piperazine-2-one (344 mg, 3.44 mmol) in CH2Cl2 (13 mL). The solution was stirred at room temperature for 16 hours, then concentrated under vacuum. The residue was dissolved in N,N-dimethylformamide (10 mL) and stirred under nitrogen as sodium hydride (60% dispersion in oil, 0.25 g, 6.25 mmol) was added at room temperature. The mixture was stirred for 30 minutes, then benzyl bromide (0.532 mL, 4.47 mmol) was added. The mixture was stirred under nitrogen for 1 hour, and the reaction was quenched by cautious addition of water (3 mL). Finally, the mixture was diluted with water (50 mL) and stirred at room temperature for 2 hours. The resulting precipitate was collected by filtration and washed with water (40 mL), then dried under vacuum to the titled compound (0.82 g, 82%). 1H NMR (400 MHz, methanol-d4) delta ppm 1.46 (s, 9H), 3.30-3.33 (m, 2H), 3.60 (t, J=5.2 Hz, 2H), 4.11 (s, 2H), 4.62 (s, 2H), 7.25-7.37 (m, 5H); MS (ESI) m/z 291 (M+H)+.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBVIE INC.; Bunnelle, William; Cowart, Marlon; Drizin, Irene; Koenig, John Robert; Pliushchev, Marina; Scanio, Marc; (80 pag.)US2016/376240; (2016); A1;,
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4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred mixture of 1-(2-propyl)piperazine (130 mg, 1.0 mmol) and dry DCM (10 ml) was added 2-(4-chlorophenoxy)ethyl 4-nitrophenylcarbonate (330 mg, 1.0 mmol). The mixture was stirred overnight at room temperature and then diluted with DCM (30 ml). The reaction mixture was washed with 0.5 N NaOH (3.x.20 ml) and water (3.x.20 ml). The organic phase was concentrated and the oily residue was dissolved in a 0.5 N HCl solution (15 ml). The acidic solution was washed with diethyl ether (10 ml), concentrated and re-evaporated twice with acetonitrile to give 300 mg (82percent) of the title compound as a solid. M.p. 174-176 1H NMR (400 MHz, DMSO-d6): 51.25 (d, 6H), 2.88-3.02 (m, 2H), 3.3-3.5 (m, 5H), 3.95-4.10 (m, 2H), 4.20 (t, 2H), 4.35 (t, 2H), 7.00 (d, 2H), 7.34 (d, 2H), 11.0 (brs, 1H).

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Dorwald, Florencio Zaragoza; Andersen, Knud Erik; Sorensen, Jan Lindy; US2004/19039; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

259808-67-8, General procedure: The appropriate carboxylic acid (1.0 equiv) is dissolved in DMF or NMP (0.03 to 0.4M) before HATU (1.1 to 1.5 equiv), or T3P (1 to 5 equiv) the corresponding amine (1.0 to 1.5 equiv) and Hunig?s base (3.0 to 5.0 equiv) are added (the addition order of the reagents may vary) The mixture is stirred at room temperature for 45 mm. to 72h. Any one of these 3 work-up procedures can be employed:1. Water or aq. ammonium chloride is added and the aq. phase is extracted with EtOAc. The combined organic phase is washed with brine, dried over MgSO4, filtered and the filtrate evaporated under reduced pressure affording the title compound which is used in the subsequent step without further purification.2. Water or aq. ammonium chloride is added and the aq. phase is extracted with EtOAc. The combined organic phase is washed with iN HCI, sat. aq. NaHCO3 and brine, dried over Na2SO4, filtered and the filtrate evaporated under reduced pressure affording the title compound which is used in the subsequent step without further purification.3. The volatiles are removed under reduced pressure and the residue is purified by flash chromatography on silica gel or by mass-directed reverse phase HPLC, affording the title compound; The intermediate is prepared according to General Procedure 1 using a solution of Intermediate A (10.0 g, 28.3 mmol) in DMF (110 mL), HATU (12.0 g, 31.6 mmol), tert-butyl 3,3- dimethylpiperazine-1-carboxylate (6.64, 31.0 mmol) and DIPEA (12.5 ml, 71.8 mmol) affording the title compound (15.38 g, quantitative yield) as a pale yellow solid, which is used directly in the next step. 1H NMR (400 MHz, DMSO-d6) 6 8.16 (dd, J = 11.0, 2.0 Hz, 1H), 8.07 – 7.97 (m, 1H), 7.82 (s, 1H), 7.76 – 7.64 (m, 1H), 7.51 (s, 1H), 3.85 (s, 2H), 3.57 – 3.38 (m, 4H), 1.52 (s, 1OH), 1.48 (s, 6H), 1.42 (s, 9H). ESI-MS m/z calc. 543.2300, found 546.10 (M+1) Retention time: 1.23 minutes using method J.

As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; LIU, Bingcan; DORICH, Stephane; DE LESELEUC, Mylene; DUPONT-GAUDET, Kristina; JAMES, Clint, Alwyn; VAILLANCOURT, Louis; BEAULIEU, Marc-Andre; STURINO, Claudio; (236 pag.)WO2018/57588; (2018); A1;,
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78818-15-2,78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 20 4-Benzyloxycarbonyl-1-[2-(1-tert-butoxycarbonyl-4-piperidyl)ethyl]-2-piperazinone According to a similar method described in Reference Example 2, oil of the title compound was obtained from 4-benzyloxycarbonyl-2-piperazinone and 1-tert-butoxy-carbonyl-4-(2-methanesulfonyloxyethyl)piperidine. 1H-NMR (CDCl3) delta: 1.00-1.25 (2H, m), 1.45 (9H, s), 1.30-1.58 (3H, m), 1.58-1.70 (2H, m), 2.56-2.78 (2H, m), 3.33 (2H, t, J=5.2 Hz), 3.38-3.50 (2H, m), 3.71 (2H, t, J=5.3 Hz), 3.97-4.20 (2H, m), 4.14 (2H, s), 5.15 (2H, s), 7.26 (5H, s). IR (KBr): 1694, 1657, 1426, 1236, 1163 cm-1.

78818-15-2 Benzyl 3-oxopiperazine-1-carboxylate 736777, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Takeda Chemical Industries, Ltd.; US6403595; (2002); B1;,
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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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

Anhydrous piperazine 1 9.5 g (0.11 mol) and piperazinium dihydrochloride 2 31.8 g (0.2 mol) were dissolved in ethanol (80 mL), and the mixture was heated at 75 C for 3 h. To the solution, benzyl chloride 13.9 g (0.11 mol) was added dropwise. The reaction mixture was refluxed for another 2 h monitoring by TLC. The stirring mixture was cooled and then filtered. The filter cake was washed with ethanol and the filtrate was concentrated in vacuo, which was then washed with a solution of NaOH (6 M, pH > 12). The aqueous layer was extracted with CH2Cl2 at pH > 12. The organic layers were combined, dried over Na2SO4, and concentrated in vacuo. The crude product was purified by flash column chromatography on silica gel (1:3 MeOH/CH2Cl2) to give N-benzylpiperazine 3 18.4 g; yield 95 %. 1HNMR (500 MHz, CDCl3): 7.34-7.28 (m, 5H, Ph), 3.57 (s, 2H, OBn), 3.23 (s, 4H, piperazine-H), 2.77 (s, 4H, piperazine-H). MS (ESI): m/z = 176 (M+ +H). Spectroscopic data are according to the literature [19]., 142-64-3

The synthetic route of 142-64-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Hu, Xiao; Qiu, Qiong; Wang, Wen-Ling; Wang, Jin; Research on Chemical Intermediates; vol. 43; 1; (2017); p. 57 – 61;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.848482-93-9,(S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

848482-93-9, To a stirred suspension of (5)-4-(tert-butoxycarbonyl) piperazine-2-carboxylic acid (1.0 g, 4.34 mmol) in water (5 rnL) was added solid NaHC03 (0.73 g, 8.68 mmol) at room temperature. The reaction mixture was stirred at room temperature to get clear solution. Solution of CBZ-CI (1.22 mL, 8.68 mmol) in 1,4-dioxane (10 mL) was added dropwise and the reaction mixture was stirred at room temperature for 16 h. The reaction mixture was diluted with water (20 mL) and extracted with EtOAc (2×20 mL). The aqueous layer was acidified with 0.5M aqueous HC1 to pH 5 and extracted with EtOAc (2×50 mL). The combined organic layers were dried over anhydrous a2S04, filtered, and concentrated under reduced pressure to afford the title compound (1.30 g) as white solid.

As the paragraph descriping shows that 848482-93-9 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; BLIZZARD, Timothy Allen; BIFTU, Tesfaye; WO2013/148478; (2013); A1;,
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Piperazines – an overview | ScienceDirect Topics