Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

STEP A: 4-(4-Bromo-2-cvano-phenyl)-piperazine-1-carboxylic acid tert-butyl ester. A mixture of 5-bromo-2-fluoro-benzonitrile (1.05g), piperazine-1 -carboxylic acid tert-butyl ester (1.08g) and Na2CO3 (1.03g) in DMF was heated to 1000C for 24h. The resulting mixture was cooled, diluted with water (50 ml_) and extracted with diethyl ether. The resulting mixture was dried over MgSO4, the solvent was removed and the resulting residue purified on SiO2 (hexanes/ EtOAc 0 to 25%) to yield the title compound., 57260-71-6

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; Janssen Pharmaceutica N.V.; WO2009/79593; (2009); A1;,
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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

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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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;,
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.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

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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Piperazines – an overview | ScienceDirect Topics

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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5308-25-8, A mixture of 5-bromo-2-nitropyridine (1.02 g, 5.02 mmol) and 1 -ethylpiperazine (1 .71 g, 15.0 mmol) in N-methyl-2-pyrrolidinone (5 mL) was stirred at 120 C for 3 h. After this time, the reaction was cooled to room temperature, poured into water (100 mL) and extracted with methylene chloride (2 chi 100 mL). The combined organic layers were dried over sodium sulfate, filtered and the filtrate concentrated under reduced pressure. The resulting residue was purified by chromatography (silica, gradient, 1 :49 methanol/methylene chloride to 1 :9 methanol/methylene chloride) to afford l-ethyl-4-(6-nitropyridin-3- yl)piperazine as a yellow solid: 1H NMR (400 MHz, DMSO- )d 8.25 (d, J = 2.8 Hz, 1 H), 8.14 (d, J = 9.2 Hz, 1H), 7.48 (dd, J = 9.2, 2.8 Hz, 1H), 3.50-3.46 (m, 4H), 2.50-2.38 (m, 4H, merged with DMSO peak), 2.37 (q, J = 7.2 Hz, 2H), 1.02 (t, J= 7.2 Hz, 3H).

5308-25-8 1-Ethylpiperazine 79196, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GILEAD SCIENCES, INC.; BLOMGREN, Peter; CURRIE, Kevin, S; KROPF, Jeffrey, E.; LEE, Seung, H.; MITCHELL, Scott, A.; SCHMITT, Aaron, C.; XU, Jianjun; ZHAO, Zhongdong; WO2011/112995; (2011); 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.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

13754-38-6, Example 18 N-{[1-(2-(4-benzoylpiperazine-1-yl)propane-1-yl)-pyrrolidine-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide 400 mg (1 . 07 mmol) N-{[1-(2-hydroxypropyl)-pyrrolidine-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide and 0.18 ml (1.29=01, 1.2 eq.) triethylamine described at manufacturing example 6 were dissolved to 20 ml dichloromethane and cooled to 3 C. under argon gas. 135 mg (1.18 mmol, 1.1 eq.) methansulfonyl chloride was slowly added to reaction solution and was stirred at same temperature for 30 min. 20 ml purified water was added and then organic layer was separated and concentrated with decompression. After 10 ml acetonitrile were added to obtained residues and dissolved them, 444 mg (3.21 mmol) potassium carbonate and 202 mg (1.06 mmol) 1-benzoylpiperazine were added. After stirring for 2 hours at room temperature, 15 ml saturated sodium chloride aqueous solution was added to reaction solution and was extracted twice with 15 ml ethylacetate. After organic layer was collected and dried with anhydrous magnesium sulfate, it was concentrated with decompression. 30 mg (51%) target compound as light-yellow solid was yielded by purifying obtained residues with chromatography using silicagel (mobile phase:dichloromethane/methanol=5:1 and 1:1). 1H NMR (400 MHz, DMSO-d6) 1.05 (3H, s), 1.55-1.65 (1H, m), 2.00-2.10 (1H, m), 2.15-2.25 (1H, m), 2.28-2.55 (9H, m), 2.70-2.85 (2H, m), 3.17 (1H, d), 3.54-3.65 (2H, m), 3.87 (2H, d), 4.10-4.20 (1H, m), 7.35-7.40 (2H, m), 7.40-7.47 (3H, m), 7.74 (1H, t), 7.92 (1H, d), 8.14 (1H, s), 8.18 (1H, d), 8.23 (1H, s), 9.01 (1H, t) MS (M)+ 545.6

The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; YANG JI CHEMICAL CO., LTD.; US2012/190689; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics