Heterocyclic Building Blocks-piperazine

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1 14 (1.60 g, 6.91 mmol) in toluene (21.1 mL) under an argon atmosphere was added (S)-/eri-butyl 2-methylpiperazine-l -carboxylate (1 15, 1.38 g, 6.91 mmol, AK Scientific, Inc., Union City, CA), sodium teri-butoxide (0.73 g, 7.60 mmol, Sigma-Aldrich), and 2-dicyclohexylphosphino-2′,4′,6′-triisopropylbiphenyl (i.e., “X-Phos,” 0.49 g, 1.04 mmol, Sigma-Aldrich). The mixture was degassed under argon and thentris(dibenzylideneacetone) dipalladium (Pd2(DBA)3, 0.63 g, 0.69 mmol, Sigma-Aldrich) was added to form a reaction mixture. The reaction mixture, heated in an oil bath maintained at temperature within the range of from 80C to 85C, was stirred for 1.5 hours. Thereafter, the mixture was cooled to a temperature of about 25C, poured onto cold water, and extracted with EtOAc. The organic layer was separated, washed with brine, and concentrated to an oil which was chromatographed on a silica gel column eluted with 10:90 EtOAc:hexanes and 20:80 EtOAc:hexanes to provide 1.71 g of 1 16 as a solid (63% yield). NMR (CDC13) delta: 1.25 (3H, d, J=6.80Hz), 1.46 (3H, s), 1.48 (9H, s), 1.53 (3H, s), 2.89 (1H, dt, J=3.29, 13.59Hz), 3.09 ( 1 H, dd, J=3.73, 12.06Hz), 3.23 (1H, dt, J=2.85, 13.59Hz), 3.69 (1H, t, J=7.89Hz), 3.83 (1 H, d, J=12.72Hz), 3.92 (1 H, d, J=13.81Hz), 4.01 (1H, d, J=12.90Hz), 4.27 (1H, t, J=6.14Hz), 4.31 (1H, brs), 5.01 (1H, t, J=7.24Hz), 7.30 (1H, d, J=1.97Hz), 7.95 (1H, s). LC/MS (M+1): m/z = 396.

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; PURDUE PHARMA L.P.; Shionogi & Co. Ltd.; TAFESSE, Laykea; ANDO, Shigeru; KUROSE, Noriyuki; WO2012/176061; (2012); 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

2-Chloro-N-methyl-N-(4-nitro-phenyl)-acetamide (210.0 g / 0.9185 mol) was suspended in toluene (1157.56 ml) and heated to 40C. N-Methylpiperazine (252.65 ml / 2.48 eq) was added dropwise within 30 minutes. The reaction was stirred for 2 hours at 55C. After cooling to ambient temperature, the reaction was washed with water (157.23 ml) and the organic layer diluted with iPrOH (1075.33 ml). Pd/C (18.81 g) was added and the reaction hydrogenated with ? (lbar) at 20C over night. After complete conversion the catalyst was filtered off, the filtrate concentrated to ~ 150 ml and triturated with Et20 (120.0 ml). The crystalline product was filtered off, washed with Et20 and dried under vacuum to obtain 170 g (70.5 %) of N-(4-amino-phenyl)-N-methyl-2-(4-methyl-piperazin-l-yl)-acetamide.

109-01-3, The synthetic route of 109-01-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; RATIOPHARM GMBH; TEVA PHARMACEUTICALS USA, INC.; ALBRECHT, Wolfgang; FISCHER, Dirk; JANSSEN, Christian; WO2012/68441; (2012); A2;,
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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.

Ethyl-7-r(2S)-4-(tgrt-butoxycarbonyl)-2-(hydroxymethvDpiperazin-l-vn-l- cyclopropyl-6-fluoro-8-formyl-4-oxo-l,4-dihvdroquinoline-3-carboxylate (3)tert-Butyl-(3S)-3-(hydroxymethyl)piperazine-l-carboxylate (1) (0.543 g,0.00251 mol) and N-methylpyrrolidinone (20 mL) were added to a 40 mL vial. Ethyl- 1 -cyclopropyl-6,7-difluoro-8-formyl-4-oxo- 1 ,4-dihydroquinoline-3-carboxylate (2) (0.807 g, 0.00251 mol) and N,N-diisopropylethylamine (1.31 mL, 0.00753 mol) were added and the reaction was heated at 50 C overnight. The reaction was checked by HPLC and LC/MS and was shown to be -50% complete. The heat was increased to 75 C overnight. HPLC showed the reaction to be -85% complete with an impurity forming. The reaction was stopped and the mixture was diluted with water. The aqueous was extracted with ethyl acetate (3 x 150 mL). The combined organic layers were washed with water (3 x 50 mL) and brine (25 mL). The organic layer was then dried with sodium sulfate, filtered and concentrated in vacuo. The crude material was purified by silica gel chromatography on 120 g of silica gel using 15% to 50% acetone in dichloromethane as the eluent to afford 800 mg (62%) of the desired product (3) as a yellow solid. MS ES+ 518.2 m/z for [C26H32FN307+H]+; MS ES” 516.2 m/z for [C26H32FN307-H], 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ACHAOGEN, INC.; WAGMAN, Allan, Scott; MOSER, Heinz, Ernst; MCENROE, Glenn, A.; AGGEN, James, Bradley; LINSELL, Martin, Sheringham; GOLDBLUM, Adam, Aaron; SIMONS, Lloyd, J.; BELLIOTTI, Thomas, R.; HARRIS, Christina, R.; POEL, Toni-Jo; MELNICK, Michael, J.; GASTON, Ricky, D.; GRIFFIN, John, H.; WO2011/31740; (2011); A1;,
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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

5464-12-0, Compound 31g S6-2d was added to the reaction flask under nitrogen protection.33g 1-hydroxyethyl-4-methylpiperazine, 60g of triphenylphosphine, inject 625mL of toluene, stir to dissolve, and then add52.7 g of di-tert-butyl azodicarboxylate,The reaction was heated to 50¡ãC and stirred for 2 hours.TLC showed that the compound S6-2d was completely reacted to produce the product S6-2e with increased polarity. After the treatment, 30percent hydrochloric acid in methanol was added and 300 mL was stirred at room temperature for two hours.Filtrate the filtrate,The cake was beaten with methyl tert-butyl ether to give a filtrate.Combine the filtrate dry powder mix,Column chromatography (dichloromethane/methanol=15/1) gave 22 g of a yellow liquid.That is, compound S6-2e with a yield of 57percent

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

Reference£º
Patent; Douchuang (Shanghai) Pharmaceutical Technology Co., Ltd.; Wang Lei; Wang Xiaolei; Wang Zongying; Chen Da; Cao Ruqi; (20 pag.)CN107573360; (2018); A;,
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Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Benzyl chloroformate (3.40 ml, 24.00 mmol) was slowly added to an ice-cold stirred solution of 1-(2-hydroxyethyl)piperazine (2.60 g, 20.00 mmol) and DIEA (7.0 ml, 40.0 mmol) in dichloromethane (75 ml). The mixture was allowed to warm to room temperature and stirred for 24 h then concentrated in vacuo. The residue was purified by (eluant 6% methanol/chloroform) to give a colourless gum identified as benzyl 4-(2-hydroxyethyl)piperazine-1-carboxylate (4.80 g, 91%).

103-76-4, 103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Ferring B.V.; EP1449844; (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.138775-02-7,(R)-4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

(2,S)-4-Benzyloxycarbonyl-l-/er/-butoxycarbonyl-piperazine-2-carboxylic acid (5.0 g, 13.72 mmol) was dissolved in anhydrous THF (70 mL) and cooled to 0 C with an ice bath. Borane dimethyl sulfide complex (2.6 mL, 27.44 mmol) was added dropwise at 0 C, slowly. Then the reaction solution was left to warm up to room temperature and stirred overnight. The reaction mixture was then cooled to 0 C with an ice bath and quenched with water, dropwise, and extracted with EtOAc. The aqueous phase was extracted with DCM (2x). Combined organic layers were dried over anhydrous MgS04, filtered and evaporated under reduced pressure. It was used without further purification.

138775-02-7, As the paragraph descriping shows that 138775-02-7 is playing an increasingly important role.

Reference£º
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; ALTAS TAHIROVIC, Yesim; WILSON, Lawrence; PELLY, Stephen Christopher; (102 pag.)WO2019/183133; (2019); A1;,
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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, In a sealed tube, 2-(2,8-dimethylimidazo[l,2-b]pyridazin-6-yl)-7-fluoro-9-methyl- pyrido[l,2-a]pyrimidin-4-one (Intermediate 4; 50 mg, 0.155 mmol) and (R)-2-methylpiperazine (62 mg, 0.619 mmol, 4.0 eq.) were stirred in DMSO (2 mL) at 125C overnight. The solvent was removed under high vacuum. The residue was taken up in CH2CI2and washed with an aqueous saturated solution of NaHC03. The organic layer was separated and dried over Na2S04and concentrated in vacuo. The crude was purified by column chromatography (S1O2,CH2Cl2/MeOH=95/5 to 90/10) to afford the title product (40 mg, 70%) as a light yellow solid. MS m/z 404.3 [M+H+].

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

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; MCCARTHY, Kathleen Dorothy; METZGER, Friedrich; RATNI, Hasane; (76 pag.)WO2017/81111; (2017); A1;,
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163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (R) -tert-butyl3-methylpiperazine-1-carboxylate (500 mg, 2.5 mmol) and triethylamine (700 mg,6.3 mmol) in DCM (10 mL) was added methylsulfamoyl chloride (0.39 mL,4.99 mmol) at 0 dropwise. The mixture was stirred at rt for 8 h, and washedwith water (10 mL ¡Á 3) . The combined organic layer were dried over anhydrousNa2SO4 and concentrated. The residue was purified bysilica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 2/1 to give(R) -tert-butyl 3-methyl-4- (methylsulfonyl) piperazine-1-carboxylate as awhite solid (444 mg, 63) . 1H NMR (400 MHz, CDCl3): delta ppm 4.04-4.24 (m, 2H) , 3.82-3.98 (m, 1H) , 3.54 (d, J 12.7 Hz, 1H) ,3.14-3.21 (m, 1H) , 3.04-3.18 (m, 1H) , 2.87-3.00 (m, 1H) , 2.88 (s, 3H) , 1.48(s, 9H) , 1.26 (d, J 6.8 Hz, 3H) and MS-ESI: m/z 223.15 [M-55] +., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); 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.

Intermediate 1 Preparation of N,N-Bis-Cbz-2-carboxypiperazine To a mixture of 2-carboxypiperazine dihydrochloride (5.08 g, 25 mmol), 1,3-dioxolane (45 ML), and water (30 ML) at 0 C. was added 50% aqueous sodium hydroxide (NaOH) (6 ML) dropwise.benzyl chloroformate (BzCOCl) (7.8 ML, 55 mmol) then was added to the resulting mixture dropwise in alternating portions with 50% aqueous sodium hydroxide (4 ML) in order to maintain a PH between 8-11.The temperature of the reaction was maintained below 15 C. during a 30-minute addition period.The resulting biphasic mixture was stirred at 0 C. for an additional 30 minutes, after which the reaction was acidified to PH 2 with 2 N hydrochloric acid (HCl), then diluted with ethyl acetate (100 ML).The organic layer was washed with brine (2*10 ML), and the aqueous phase was reextracted with ethyl acetate (20 ML).The combined organic extracts then were dried over sodium sulfate (Na2SO4), filtered, and concentrated under reduced pressure.The residue was purified by flash column chromatography, eluding with methylene chloride/methanol (40:1 to 10:1), to provide the bis-protected piperazine as a white solid (7.0 g, 70%): TLC Rf (10:1 methylene chloride/methanol)=0.55; 1H NMR (300 MHz, DMSO-d6) delta7.40-7.20 (m, 10H), 5.01-5.27 (m, 4H), 4.92-4.60 (m, 2H), 4.20-3.81 (m, 2H), 3.40-2.82 (m, 3H)., 3022-15-9

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

Reference£º
Patent; Orme, Mark W; Sawyer, Jason Scott; US2003/225093; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 1 from Method X (50 mg) was dissolved in anhydrous dichloromethane (3 mL) and treated with 41 mg of tert-butyl 2-methylpiperazine- 1 – carboxylate. To the resulting solution was added activated 4 A molecular sieves, and the mixture was stirred 2 hrs at room temperature. 33 mg of sodium triacetoxy borohydride was added, and the reaction was stirred overnight, after which it was diluted with dichloromethane, washed with water and brine, and dried over MgS04 to yield the title compound.

120737-78-2, As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Patent; UNIVERSITY OF ROCHESTER; BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA; GELBARD, Harris A.; DEWHURST, Stephen; GENDELMAN, Howard E.; WO2014/85795; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics