Heterocyclic Building Blocks-piperazine

74879-18-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of bromobenzene (300 mg), (S)-2-methylpiperazine (230 mg), (S)-(-)-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (BINAP) (48 mg), sodium tert-butoxide (266 mg), tris-(dibenzylideneacetone)dipalladium(0) (26 mg) and toluene (15 ml) was stirred at 100 C. for 4 hours under a nitrogen atmosphere. The mixture was cooled to room temperature and saturated aqueous sodium hydrogencarbonate solution was added thereto. The organic layer was separated, washed with brine and dried over magnesium sulfate. The solvent was removed under reduced pressure. The obtained crude product was purified by silica gel column chromatography (chloroform-methanol 20:1) to give the title compound in a pure form. [00204] 1H-NMR (300 MHz, CDCl3) delta 1.11 (d, J=6 Hz, 3H), 2.37 (dd, J=12 Hz,1 Hz, 1H), 2.72 (td, J=12 Hz,3 Hz, 1H), 2.95-3.18 (m, 3H), 3.52 (d, J=12 Hz, 2H), 6.82-6.98 (m, 3H), 7.22-7.29 (m,2H).

The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Fujisawa Pharmaceutical Co., Ltd.; US6825200; (2004); B1;,
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.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1 : A mixture of lb (4.85g, 16.5mmol) and 9a (16.5g, 0.33mol) in ethanol (50mL) was heated under reflux overnight, then evaporated under high vacuum. The residue was re-dissolved in ethanol and the resulting precipitate was filtered off. The filtrate was concentrated and dried to give crude 9b (4.02g, ca. 100percent).

655225-01-7, As the paragraph descriping shows that 655225-01-7 is playing an increasingly important role.

Reference£º
Patent; TYROGENEX, INC.; LIANG, Congxin; WO2011/41399; (2011); 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.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

5271-27-2, EXAMPLE-5 Preparation of 1,2,3,4,10,14b-hexahydro-2-methyl-pyrazino[2,1-a] pyrido{2,3-c} [2]Benzazepine of Formula 17: 1-Methyl-3-phenylpiperazine (50.0 g, 0.284 mol) was heated with 2-chloro-3-cyanopyridine (39.35 g, 0.284 mol) in the presence of potassium fluoride (49.51 g, 0.852 mol) and N,N-dimethylformamide (750.0 ml) as a solvent for 30.0 hrs at 148-154¡ã C., followed by quenching with water and extraction with ethyl acetate gave 1-(3-cyanopyridyl-2-)-4-methyl-2-phenylpiperazine (70.0 g). 1-(3-Cyanopyridyl-2)-4-methyl-2-phenylpiperazine on hydrolysis with saturated alcoholic potassium hydroxide solution (850.0 ml) at 80-85¡ã C. followed by extraction with chloroform gave 1-(3-carboxypyridyl-2)-4-methyl-2-phenylpiperazine (20.0 g).

The synthetic route of 5271-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sebastian, Sonny; Patel, Hetal Virendra; Thennati, Rajamannar; US2002/95038; (2002); A1;,
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21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

This compound was prepared by treatment of a solution of 2-(3,4-dimethoxyphenyl)ethanol (1.82 g, 10 mmol) in DCM (30 ml) with pyridine (1.6 ml) and then with a solution of 4-nitrophenyl chloroformate (2.0 g, 10 mmol) in DCM (25 ml). The mixture was stirred at room temperature for 2 hours, and was then washed with dilute hydrochloric acid and with water. After drying with magnesium sulfate the solution of the crude carbonate was concentrated, to yield 3.8 g of a yellow oil. To a solution of 0.69 g (2 mmol) of this oil in acetonitrile (10 ml) was added 1-cyclopentylpiperazine (0.6 g, 4 mmol). The resulting mixture was stirred at room temperature for 2 days, concentrated under reduced pressure, and the residue was redissolved in DCM and extracted with dilute hydrochloric acid. The aqueous phase was made alkaline by addition of solid NaHCO3, and extracted three times with DCM. The combined extracts were dried over magnesium sulphate, concentrated, and the residue was redissolved in 1 M hydrochloric acid (5 ml) and ethanol. The mixture was concentrated, and the residue recrystallized from ethanol, to yield 82 mg of the title compound as colorless solid. 1H NMR (DMSO-d6), 1.53 (m, 2H), 1.65-1.83 (m, 4H), 1.98 (m, 2H), 2.82 (t, J=7 Hz, 2H), 2.85-3.00 (m, 2H), 3.24-3.49 (m, 5H), 3.71 (s, 3H), 3.74 (s, 3H), 4.01 (m, 2H), 4.21 (t, J=7 Hz, 2H), 6.74 (m, 1H), 6.87 (m, 2H), 11.05 (br s, 1H)., 21043-40-3

21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Dorwald, Florencio Zaragoza; Andersen, Knud Erik; Sorensen, Jan Lindy; US2004/19039; (2004); A1;,
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57184-25-5, 1-(Cyclopropylmethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57184-25-5, 9.8 g (33.4 mmol) of 4-dibenzylcyclohexanone was dissolved in 100 mL dichloromethane and stirred for 12 h at RT with 5.6 g (40 mmol) of N-cyclopropylmethylpiperazine and 8.5 g (40 mmol) of NaBH(OAc)3. Then water and potassium carbonate were added, the org. phase was separated off, dried and the solvent was eliminated in vacuo. The residue was purified over a silica gel column (about 50 mL silica gel, about 3 L ethyl acetate 95/methanol 5+0.25% conc. ammonia. The appropriate fractions were evaporated down in vacuo. The faster eluting cis compound crystallised from ethyl acetate. The trans-compound was crystallised from ethanol+conc. HCl. Yield: 8.5 g (61%) cis-isomer and 2.2 (13%) trans-isomer.

The synthetic route of 57184-25-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Boehringer Ingelheim Pharma GmbH Co. KG; US2004/176380; (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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, 0.62g to 1.0g of Intermediate VI and cyclopropylmethyl – piperazin-1-yl – methyl ketone was added to a 100mL one-neck flask was added10mLDMF clear solution was stirred, then add 2.05gHBTU, 0.82g triethylamine, room temperature for 5h. After completion of the reaction the reactionIt was poured into water, extracted with ethyl acetate, dried over anhydrous sodium sulfate spin column chromatography to give 1.1g solid.

59878-57-8 1-(Cyclopropylcarbonyl)piperazine 2064235, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Warwick Nanjing Pharmaceutical Technology Co., Ltd.; Zhang, Xiaoqing; Song, Zhinchun; Bao, Jinyuan; Jiang, Yuwei; (25 pag.)CN105254628; (2016); A;,
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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.

To a mixture of 3-(6-bromo-quinazolin-4-yl)-5-fluoro-benzoic acid (1.36 g, 3.72 mmol) in CH2CI2 (15 mL) was added DIPEA (1.30 mL, 7.44 mmol) and HBTU (1.694 g, 4.47 mmol) at rt. The reaction mixture was stirred at rt for 20 min. To the mixture was then added 1- (piperazin-l-yl)ethanone (0.572 g, 4.47 mmol) and the reaction mixture was stirred at rt for 1 h. The reaction was quenched with a saturated aqueous solution of NaHC03 and extracted with CH2CI2. The organic layer was washed twice with brine, dried by passing through a phase separating cartridge and evaporated. Purification by Flash chromatography using Biotage Isolera system (amine functionalized silica KP-NH, eluting with Cyclohexane/EtOAc 0 to 100%) gave the title compound (1.20 g, 68% yield) as a beige foam. MS: 457.4-459.3 [M+1]+, Rt(2,) = 1.03 min.

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

Reference£º
Patent; NOVARTIS AG; COOKE, Nigel Graham; FERNANDES GOMES DOS SANTOS, Paulo Antonio; FURET, Pascal; HEBACH, Christina; HOeGENAUER, Klemens; HOLLINGWORTH, Gregory; KALIS, Christoph; LEWIS, Ian; SMITH, Alexander Baxter; SOLDERMANN, Nicolas; STAUFFER, Frederic; STRANG, Ross; STOWASSER, Frank; TUFILLI, Nicola; VON MATT, Anette; WOLF, Romain; ZECRI, Frederic; WO2013/88404; (2013); A1;,
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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.,934-98-5

(iii) tert-Butyl (3,5-dimethoxy-4-((2-(4-methylpiperazin-1-yl)ethyl)carbamoyl)phenyl) carbamate HATU (700 mg, 1.841 mmol) was added to a solution of the product from step (ii) above (400 mg, 1.345 mmol), 2-(4-methylpiperazin-1-yl)ethanamine (300 mg, 2.095 mmol) and Hunig’s base (700 mu, 4.01 mmol) in DCM (5 mL). The reaction mixture was stirred at rt for 16h. The mixture was partitioned between DCM (15 mL) and water (15 mL). The organics were separated, dried (MgSCU) filtered and evaporated to give a yellow gum which was pre- absorbed onto silica (4 g) and purified by chromatography on silica gel (12 g column, 2percent MeOH:DCM to 10percent) to afford the sub-title compound (410 mg) as a pale yellow glass. 1 H NMR (400 MHz, DMSO-d6) delta 9.37 (s, 1 H), 7.72 (t, 1 H), 6.83 (s, 2H), 3.66 (s, 6H), 3.28 – 3.15 (m, 2H), 2.48 – 2.25 (m, 10H), 2.17 (s, 3H), 1.48 (s, 9H). LCMS m/z 423 (M+H)+ (ES+)

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; RESPIVERT LIMITED; TOPIVERT PHARMA LIMITED; BAKER, Thomas Matthew; FYFE, Matthew Colin Thor; JONES, Geraint; THOM, Stephen Malcolm; (270 pag.)WO2016/51187; (2016); A1;,
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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 solution of 7-benzyl-2,4-dichloro-6,8- dihydro-5H-pyrido[3,4-d] pyrimidine (2.00 g, 6.80 mmol, 1.00 eq) in DMSO (40.0 mL) was added DIEA (1.76 g, 13.6 mmol, 2.38 mL, 2.00 eq) and 1-tert-butyl 2-methylpiperazine-l,2- dicarboxylate (1.74 g, 7.14 mmol, 1.05 eq). The mixture was stirred at 55 C for 16 hours. The mixture was diluted with water (100 mL) and extracted with ethyl acetate (3 x 100 mL). The combined organic layers were washed with brine (3 chi 100 mL), dried over Na2S04, filtered and concentrated to dryness. The residue was purified by column chromatography (S1O2, diethyl ether/ethyl acetate = 1 :0 to 3 : 1) to give 1-tert-butyl 2-methyl-4-(7-benzyl-2-chloro-6,8-dihydro- 5H-pyrido[3,4-d]pyrimidin -4-yl)piperazine-l,2-dicarboxylate (3.10 g, 5.70 mmol, 83.8 % yield, 92.3 % purity) as a yellow semisolid. ESI MS m/z 502.2 [M+H]+.

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

Reference£º
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); A1;,
Piperazine – Wikipedia
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34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(i) 2-Methoxy-4-(4-methyl-2-oxopiperazin-l-yl) benzaldehvde To a solution of 4-bromo-2-methoxybezaldehyde (10.0 g, 46.5 mmol) in 1 ,4-dioxane (140 mL) was added Cul (8.84 g, 46.5 mmol), N,N’-dimethyldiaminoethane (10.0 mL, 93.0 mmol), 4-methylpiperazin-2-one (7.95 g, 69.8 mmol), and Cs2C03 (45.0 g, 139 mmol). The mixture was heated to 100C and stirred for 5h. After cooling, the mixture was filtered, and the solution was adjusted to pH 2~3 with IN HCl. After stirring for 3h at r.t., the mixture was neutralized with sat. aq. NaHC03,and the resulting mixture was extracted with EtOAc. The combined organic solutions were washed with brine, and then dried (Na2S04). After removal of the solvent in vacuo, the subtitle compound was obtained as a white solid (10.7 g, 43.1 mmol, 93%); NMR: 10.4 (1H, s), 7.86 (1H, d), 7.1 1 (1 H, d), 6.92 (1H, dd), 3.92 (3H, s),3.76 (2H, t), 3.30 (2H, s), 2.82 (2H, t), 2.42 (3H, s); LC-MS: m/z = 249 [MH+] (T = 0.92 min).

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Dainippon Sumitomo Pharma Co., Ltd.; ASTRAZENECA AKTIEBOLAG; TOSAKI, Shinya; HORI, Seiji; WO2012/67268; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics