Month: April 2021

54699-92-2, 4-Methyl-1-piperazineacetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

54699-92-2, Example 13; General Method for the Preparation of Active Esters of N-Substituted Piperazine Acetic Acid from Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH2-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

54699-92-2 4-Methyl-1-piperazineacetic acid 2762732, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Applera Corporation.; US2005/148771; (2005); A1;; ; Patent; Applera Corporation.; US2005/148774; (2005); A1;,
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39539-66-7, 4-Methylpiperazine-1-carbonyl chloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 5,6-dimethyl-2-(3-fluorophenyl)-3-hydroxyisoindolin-1-one (83 mg, 0.31 mmol) in anhydrous dimethylformamide (3 ml) was added to a suspension of 65% sodium hydride (13 mg, 0.34 mmol) in anhydrous dimethylformamide (3 ml), and stirred at 25C for 35 minutes. Then, a solution of 1-chlorocarbonyl-4-methylpiperazine (50 mg, 0.31 mmol) in anhydrous dimethylformamide was added thereto, and stirred with heating at 70C for 5 hrs. The reaction solution was concentrated under reduced pressure, and water was added to the residue, followed by extracting with chloroform. The extract was concentrated under reduced pressure, and the residue was purified by silica gel chromatography (chloroform: methanol = 20: 1). The resulting crystals were washed with petroleum ether to give 21 mg of the title compound. melting point: 146-148C 1H-NMR (CDCl3) delta: 2.38 (3H, s, CH3), 2.40 (3H, s, CH3), 2.73 (3H, s, NCH3), 3.01-3.14 (6H, m, piperazine), 3.18-3.24 (1H, m, piperazine), 3.32-3.38 (1H, m, piperazine), 6.43 (1H, s, CH), 6.85-6.91 (1H, m, PhH), 7.33-7.39 (1H, m, PhH), 7.36 (1H, s, C4-H), 7.66 (1H, s, C7-H), 7.66-7.76 (2H, m, PhH), 39539-66-7

39539-66-7 4-Methylpiperazine-1-carbonyl chloride 3016935, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Maruishi Pharmaceutical Co., Ltd.; EP1566378; (2005); A1;,
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109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

HATU (0.207 g, 0.544 mmol) was added to a solution of 3-chloro-6-(1 H- pyrazol-4-yl)-8-(trifluoromethyl)imidazo[1 ,2-a]pyridine-2-carboxylic acid (0.150 g, 0.454 mmol), 1-methyl-2-piperazinone hydrochloride (0.068 g, 0.454 mmol) and DIPEA (0. 74 mL, 0.998 mmol) in DMF (1.5 mL). The mixture was stirred at room temperature overnight. The reaction mixture was diluted with ethyl acetate and washed with water. The organic layer was dried over sodium sulfate and the solvent was evaporated. The residue was purified by reverse phase HPLC (acetonitrile/water with 0.1 % formic acid) to afford 0.020 g (9%) of the title compound as a white solid. 1H NMR (400 MHz, DMSO-c/6) delta ppm 8.74 (s, 1 H) 8.18 – 8.49 (m, 2 H) 7.94 – 8.18 (m, 1 H) 4.10 – 4.63 (m, 2 H) 3.81 – 4.10 (m, 2 H) 3.39 (t, J=5.40 Hz, 2 H) 2.86 (s, 3 H). ES-LCMS m/z: 427 (M+1 ).

109384-27-2, The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; PEAT, Andrew, James; PRICE, Daniel, J.; SHOTWELL, John, Brad; TAI, Vincent; ZHANG, Huichang; WO2011/41713; (2011); A2;,
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103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

131.5 g of N-hydroxyethylpiperazine (purity 99%, about 1 mol)And 30% (mass concentration) aqueous sodium vinyl sulfonate solution (containing 1.05 mol of sodium vinyl sulfonate)Was added to a 1000 mL four-necked flask equipped with a reflux tube,The addition reaction is carried out with sufficient stirring;The reaction was carried out at 60 C for 1.0 hour,And then gradually heated to boiling reflux (about 100 ~ 120 , depending on the composition of the reaction and change)And continue to react for 2.0 hours;then,Cooled to give a reaction mother liquorcontaining 4-hydroxyethylpiperazineethanesulfonate.By high performance liquid chromatography,The yield of sodium 4-hydroxyethylpiperazineethanesulfonate was calculated to be 95.2%.A reaction mother liquor containing 0.5 mol HEPES-Na at a mass concentration of 40 wt% was placed in a 500 mL beaker,Under stirring,At room temperature,27.3 g of oxalic acid (99 wt%) was added slowly,Then stir,And acidified at 20 C for 1 hour.Into the low temperature thermostat,Cooling to 10 ,Cooling crystallization for 0.5 hours,The precipitated sodium oxalate was removed by filtration.The filtrate was placed in a beaker,Constantly stirring,1.0 g of Ba (OH) 2 was slowly added,Reaction for 1 hour,Remove the sulfate.Adding 5 g of activated carbon decolorization and filtering by filtration to obtain the filtrate,By rotary evaporation to anhydrous,To obtain a solid primary purified product.The solids were washed three times with 500 ml of ethanol,And then vacuum drying,Get high purity HEPES.

103-76-4, As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference£º
Patent; Shandong University of Technology; Cui Hongyou; Wang Jiangang; Zhu Liwei; Liu Ransheng; Yang Yong; Wang Yang; (8 pag.)CN104803949; (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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl 3-(2-chloropyrimidin-4-yl)-5-fluoro-lH-indole-l- carboxylate (400 mg, 1.15 mmol) in dioxane (1 mL), were added cesium carbonate (2.25 g, 6.90 mmol), XANTPetaOS (39.8 mg, 0.069 mmol), l-(4-Amino-phenyl)-piperazine-4-carboxylic acid tert-butyl ester (604 mg, 1.72 mmol), and bis(dibenzylideneacetone)palladium (0) (21.1 mg, 0.023 mmol). The reaction mixture vial was capped and heated to 1000C for 12 hr. The reaction mixture was cooled, diluted with H2O, and extracted with EtOAc. The organic layer was collected, dried with MgSO4, filtered, and concentrated under reduced pressure. Column chromatography (100 % Hex to 100% EtOAc produced tert-butyl 3-[2-({4-[4-(tert- butoxycarbonyl)piperazin- 1 -yl]phenyl} amino)pyrimidin-4-yl]-5-fluoro- li/-indole- 1 -carboxylate. LRMS m/z (M+H) Calcd: 589.3, found: 589.3.

170911-92-9, The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK & CO., INC.; WO2007/149427; (2007); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Preparation of ethyl 2-(4-methyl-3-oxopiperazin-1-yl)-2-phenylacetate (I50) DIPEA (0.52 ml, 2.96 mmol) and 1-methylpiperazin-2-one hydrochloride (0.22 g, 1.48 mmol) were sequentially added to a solution of ethyl 2-bromo-2-phenylacetate (0.22 ml, 1.23 mmol) in acetonitrile (4 ml). The reaction was stirred at room temperature for 1.5 hours. DIPEA (0.13 ml, 0.74 mmol) was added again and the reaction was stirred at room temperature overnight. The solvent was evaporated and the crude was purified by flash chromatography (DCM/Acetone=9/1) to obtain ethyl 2-(4-methyl-3-oxopiperazin-1-yl)-2-phenylacetate (256 mg, 75% yield) as a yellow oil. 1H NMR (300 MHz, DMSO-d6) ppm 6.91-7.66 (m, 5H), 4.28 (s, 1H), 3.99-4.22 (m, 2H), 3.23 (t, 2H), 3.00 (s, 2H), 2.80 (s, 3H), 2.61-2.71 (m, 2H), 1.14 (t, 3H).

109384-27-2, The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chiesi Farmaceutici S.p.A.; AMARI, Gabriele; Pesenti, Cristina; Bossolo, Stefano; US2013/172302; (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, General method F; A mixture of the appropriate sulfinyl derivative such as Intermediate 39 described hereinbefore (ex:2-methanesulfinyl-5-(3-trifluoromethoxy-phenyl)-imidazo[2, 1 – b][1 ,3,4]thiadiazole) (1 equiv), the appropriate amine (1.5 equiv) (ex: 2-(4-methyl- piperazin-1 -yl)-ethylamine) and Et3N (2 equiv) (0.092 mL, 0.662 mmol) in isopropanol (15 mL/mmol) was heated in a sealed tube at 110 ¡ãC for 40 h. On cooling, DCM was added and the mixture was washed with water. The organic layer was dried (sodium sulfate), filtered and concentrated. The residue was purified by column chromatography (Isolute/Flash, Sill, 0percent to 20percent MeOH in DCM) to give the desired product (ex: [2-(4-methyl-piperazin-1 -yl)-ethyl]-[5-(3- trifluoromethoxy-phenyl)-imidazo[2,1-b][1 ,3,4]thiadiazol-2-yl]-amine).; Example 47; [2-(4- ethyl-piperazin-1-yl)-ethyl]-[5-(3-trifluoromethoxy-phenyl)- imidazo[2,1-b][1,3,4]t iadiazol-2-yl]-amine; HPLC-MS (method 1): Rt= 3.15 min, [M+1]+ m/z 427.2.1H NMR (300 MHz, MeOD) delta 7.99 (s, 1 H), 7.85 (d, J = 8.0 Hz, 1 H), 7.48 (s, 1 H), 7.46 (t, J = 8.1 Hz, 1 H), 7.15 (d, J = 8.2 Hz, 1 H), 3.57 (t, J = 6.5 Hz, 2H), 2.69 (t, J = 6.5 Hz, 2H), 2.60 (m, 4H), 2.50 (m, 4H), 2.27 (s, 3H).Yield: 48percent

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

Reference£º
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); PASTOR FERNANDEZ, Joaquin; GARCIA COLLAZO, Ana, Maria; NOYA MARINO, Beatriz; GONZALEZ CANTALAPIEDRA, Esther; WO2012/20217; (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.928025-56-3,(S)-tert-Butyl 3-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

[Step 1] tert-Butyl (3S)-3-ethyl-4-methylpiperazine-1-carboxylate To a solution of tert-butyl (3S)-3-ethyl piperazine-1-carboxylate (2.0 g) in dichloromethane (20 ml), a 37% aqueous solution of formalin (3.4 ml) was added at room temperature. The reaction solution was ice-cooled and sodium triacetoxyborohydride (3.0 g) was added thereto. After that, the temperature of the reaction solution was gradually returned to room temperature and the reaction solution was stirred for 4 hours. To the reaction solution, a 1 N aqueous solution of sodium hydroxide (50 ml) was added. The reaction solution was stirred and dichloromethane and water were added, and the layers were separated. The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated. The residue was purified by silica gel column chromatography (0-10% methanol/dichloromethane) to obtain the title compound (2.14 g) as an oily substance. 1H-NMR (CDCl3) delta: 4.04-3.69 (2H, m), 3.05 (1H, t, J=11.0 Hz), 2.90-2.53 (2H, m), 2.29 (3H, s), 2.24-2.13 (1H, m), 1.94-1.85 (1H, m), 1.74-1.62 (1H, m), 1.49-1.30 (10H, m), 0.92 (3H, t, J=7.9 Hz). MS (ESI/APCI) m/z: 229 [M+H]+

928025-56-3, 928025-56-3 (S)-tert-Butyl 3-ethylpiperazine-1-carboxylate 24820542, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Daiichi Sankyo Company, Limited; Ota, Masahiro; Inoue, Hidekazu; Kawai, Junya; Ohki, Hitoshi; Toki, Tadashi; (25 pag.)US2019/284198; (2019); A1;,
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Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

REFERENCE EXAMPLE 23 4-(4-Methyl-1-piperazinyl)benzonitrile According to a similar manner to that in Reference Example 12, the title compound was synthesised from 4-fluorobenzonitrile and 1-methylpiperazine. 1 H-NMR (CDCl3) delta (ppm): 2.35(3H, s), 2.52-2.59(4H, m), 3.31-3.39(4H, m), 6.86(2H, d, J=8.9 Hz), 7.49(2H, d, J=8.9 Hz)., 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; Kyowa Hakko Kogyo Co., Ltd.; US6127541; (2000); A;,
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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, Triethylamine (5.51 g, 4 mL, 54.6 mmol, 2.7 eq) is added to a solution of 6-chloro- nicotinonitrile (2.76 g, 20 mmol, 1 eq), (i?)-2-methyl- piperazine (2.0Og, 20 mmol, 1 eq) in DMF (15 mL), and the resulting solution is stirred at rt for 36 h. A white precipitate of triethylamine hydrochloride forms in the course of the reaction. Water (15 mL) and EtOAc (100 mL) are added, the organic layer is separated, dried over sodium sulfate and concentrated under reduced pressure to a white residue. The solid is further dried under high vacuum to yield the desired product as a white solid (2.3 g, 59percent). IH NMR (400 MHz, CHLOROFORM-*/) delta ppm 8.32 (d, J=2.40 Hz, 1 H), 7.52 (dd, J=9.09, 2.27 Hz, 1 H), 6.52 (d, J=8.97 Hz, 1 H), 4.14 – 4.24 (m, 2 H), 3.01 – 3.07 (m, 1 H), 2.72 – 2.94 (m, 3 H), 2.52 (dd, J=12.76, 10.36 Hz, 1 H), 1.07 (d, J=6.32 Hz, 3 H).

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

Reference£º
Patent; NOVARTIS AG; WO2008/110611; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics