Category: piperazines

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;,
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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;,
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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.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.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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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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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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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: To a mixture of 1-benzoylpiperazine (1.0 eq) and potassium carbonate (2.0 eq) in dimethylformamide was added dropwise a solution of the corresponding substituted 9-bromo-9H-fluorene (1.0 eq) in dimethylformamide (The synthesis of 9-bromo-9H-fluorene derivatives is reported in supporting information). After stirring for 24 h at room temperature, solvent was removed and the crude residue was dissolved in diethyl ether, washed with brine, dried over magnesium sulfate,filtered and concentrated under vacuum. The residue was purified by flash chromatography as indicated in each case to afford the title compound. Reagents: 1-Benzoylpiperazine (0.23 mmol, 44 mg), potassium carbonate (0.46 mmol, 64 mg) and 3-(benzyloxy)-9-bromo-9H-fluorene (0.23 mmol, 81 mg). The crude product was purified by flash chromatography (gradient, 100% petroleum ether to 100% ethyl acetate in 15 min) to afford a yellow oil (54.3 mg, 50%). TLC Rf: 0.40 (petroleum ether/ethyl acetate 80/20). IR (cm-1): 697, 710, 770, 1001, 1017, 1186, 1257, 1278, 1427, 1448, 1488, 1578, 1628, 2851, 2920. HPLC: method 2, rt = 3.65 min, purity 98%. 1H NMR (300 MHz, CDCl3) delta (ppm): 2.45 (bs, 2H); 2.86 (bs, 2H); 3.38 (bs, 2H); 3.83 (bs, 2H); 4.86 (s, 1H); 5.18 (s, 2H); 6.97 (dd, J = 2.4 Hz, 8.1 Hz, 1H); 7.34 (td, J = 2.1 Hz, 7.8 Hz, 2H); 7.37-7.48 (m, 9H); 7.51 (s, 1H); 7.53 (t, J = 8.4 Hz, 2H); 7.65 (t, J = 8.1 Hz, 2H). 13C NMR (75 MHz, CDCl3) delta (ppm): 42.9 (CH2); 48.6 (2 * CH2); 49.5 (CH2); 69.4 (CH2); 70.4 (CH2); 106.3 (CH); 113.8 (CH); 119.8 (CH); 125.9 (CH); 126.6 (CH); 127.1 (2 * CH); 127.4 (CH); 127.6 (2 * CH); 128.1 (CH); 128.3 (CH); 128.4 (2 * CH); 128.7 (2 * CH); 129.6 (CH); 135.7 (C); 135.9 (C); 137.0 (C); 140.9 (C); 142.6 (C); 144.4 (C); 159.5 (C); 170.3 (C). MS (DCI/CH4) m/z: 461.22 [M+H+]. HRMS (DCI/CH4): for C31H29N2O2 [M+H+]: calcd: 461.2229; found: 461.2235., 13754-38-6

As the paragraph descriping shows that 13754-38-6 is playing an increasingly important role.

Reference£º
Article; Chollet, Aurelien; Mori, Giorgia; Menendez, Christophe; Rodriguez, Frederic; Fabing, Isabelle; Pasca, Maria Rosalia; Madacki, Jan; Kordulakova, Jana; Constant, Patricia; Quemard, Annaik; Bernardes-Genisson, Vania; Lherbet, Christian; Baltas, Michel; European Journal of Medicinal Chemistry; vol. 101; (2015); p. 218 – 235;,
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208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound 11 (248.0 mg, 1 . 0mmol) and sodium iodide (180.0 mg, 1 . 2mmol) is added to methanol (10.0 ml) and stirring, and then adding substituted amine (2.1mmol) and heating to 40 C reaction 3 – 6 hours, TLC monitoring display complete raw material reaction, concentrated, column chromatography to obtain compound 12, wherein R4 With the corresponding product in the definition of the same.

208167-83-3, 208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Yang Chunhao; Miao Zehong; Yue Zhizhou; Liang Yukun; Feng Jianming; Li Jiaxin; He Qian; (30 pag.)CN104250246; (2017); B;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of carboxylic acid (50 mmol) in DMF (0.25 mL) in a 48 position Mettler Toledo XT reaction block was added PyBOP (50 mmol, 0.2 mL of 0.3 M solution in DMF) and TEA (75 mmol, 0.05 mL of 1.5 M solution in DMF) followed by the appropriate amine build blocks (55 mmol, 0.55 ml of 1 M solution in DMF). The reactions were stirred at rt 24 h and concentrated by GeneVac HT-4 to remove all reaction mixture including excess amine and DMF. The crude mixtures were dissolved in EtOAc (1 mL) and filtered through silica-packed short-column and washed with EtOAc (3 mL). The collected organic solution was concentrated in GeneVac HT-4 and dissolved in DMSO (1 mL). DMSO solution was subjected to HTAC for pre-purification analysis, purification, and final QC., 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Hwang, Jong Yeon; Attia, Ramy R.; Carrillo, Angela K.; Connelly, Michele C.; Guy, R. Kiplin; Bioorganic and Medicinal Chemistry Letters; vol. 23; 6; (2013); p. 1891 – 1895;,
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Piperazines – an overview | ScienceDirect Topics