Month: December 2020

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.,928025-56-3

Example 114a (S)-tert-Butyl 3-Ethyl-4-(6-nitropyridin-3-yl)piperazine-1-carboxylate 114a A 250-mL single-neck round-bottomed flask equipped with a magnetic stirrer and a reflux condenser was charged with 1,4-dioxane (50 mL), 5-bromo-2-nitropyridine (2.02 g, 10 mmol), (S)-tert-butyl 3-ethylpiperazine-1-carboxylate (2.14 g, 10.0 mmol), Pd2(dba)3 (458 mg, 0.50 mmol), XantPhos (576 mg, 1.0 mmol), and cesium carbonate (6.52 g, 20 mmol). After three cycles of vacuum/argon flush, the mixture was heated at 100 C. overnight. After this time the reaction was cooled to room temperature. It was then filtered and the filtrate was evaporated under reduced pressure. The residue was purified by silica-gel column chromatography eluting with 3:1 petroleum ether/ethyl acetate to afford 114a (700 mg, 22%) as a yellow solid. MS: [M+H]+ 336

The synthetic route of 928025-56-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GENENTECH, INC.; Crawford, James John; Young, Wendy B.; US2013/116245; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59878-57-8, General procedure: Piperazine derivatives 1-3 are known.10 Piperazine derivatives 4-14 were synthesized from the commercially available appropriate monoalkylated piperazines (1.44 mmol) and 2-nitro-1H-imidazolyl-propylbromide or 3-nitro-1H-1,2,4-triazolylpropylbromide (1.485 mmol)30 in the presence of potassium carbonate (13.24 mmol) in dry acetonitrile (25 mL) as described before.10 The reaction mixture was stirred under a nitrogen atmosphere at room temperature for 48 h, then filtered to remove the inorganic salts. The organic filtrate was evaporated and the residue extracted from water-chloroform. The organic layer was separated and dried over anhydrous Na2SO4. After filtration, the solvent was evaporated and the residue purified by preparative TLC on alumina plates with ethyl acetate:petroleum ether mixture. The desired product was dissolved in ethyl acetate and converted to its HCl salt by treating with HCl gas in dry ether (1 M solution)

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Article; Papadopoulou, Maria V.; Bloomer, William D.; Rosenzweig, Howard S.; Kaiser, Marcel; Chatelain, Eric; Ioset, Jean-Robert; Bioorganic and Medicinal Chemistry; vol. 21; 21; (2013); p. 6600 – 6607;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

216144-45-5, 4-(4-Methylpiperazin-1-yl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 2806-(2 , 3-dimethylphenyl)-4-N-{[4-(4-methylpi perazin-1 -yl)phenyl]methyl}pyrim idine2,4-diamine.A mixture of 4-chloro-6-(2,3-dimethylphenyl)pyrimidin-2-amine (23 mg, 0.10mmol), [4-(4-methylpiperazin-1-yl)phenyl]methanamine (29 mg, 0.14 mmol) andHunig?s base (35 pL, 0.20 mmol) in n-butanol (1.5 mL) was heated in a sealed tube at 85C overnight. The reaction mixture was concentrated and purified by preparative H PLC. LCMS [M+H] 403.

216144-45-5, The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; THOMAS HELLEDAYS STIFTELSE FOeR MEDICINSK FORSKNING; SCOBIE, Martin; HELLEDAY, Thomas; KOOLMEISTER, Tobias; JACQUES, Sylvain; DESROSES, Matthieu; JACQUES-CORDONNIER, Marie-Caroline; WO2014/84778; (2014); 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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

74879-18-8, Example 189: Synthesis of 4-Chloro-6-[2-((R)-3-methyl-piperazin-l-yl)-benzyl amino]-4a,8a-dihydro-2H-phthalazin-l-one; 2-((R)-3-Methyl-piperazin-l-yl)-benzonitrile; A mixture 2-bromobenzonitrile (1.0 g, 5.494 mmol), (S)-(+)-2-methylpiperazine(0.60 g, 5.99 mmol), Pd2(dba)3 (0.503 g, 0.549 mmol), rac-BINAP (1.026 g, 1.648 mmol) and NaO’Bu (2.11 g, 21.976 mmol) in DMA (27 mL) was heated at 8O0C for 2.5h. The mixture was allowed to cool, diluted with EtOAc and washed with water. The organic layer was washed with sat.aq. NaHCO3, brine and dried (Na2SO4). Chromatography (EtOAc/MeOH) afforded 2-((R)-3 -methyl-piperazin- 1 -yl)-benzonitrile (540 mg) as a white solid. 1H (400 MHz, d6-DMSO) delta: ppm; m/z (M+l) 202.21.

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

Reference£º
Patent; FOREST LABORATORIES HOLDINGS LIMITED; WO2008/61108; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

STEP B; Acetyl chloride (0.216 ml, 3.04 mmol) was added to a stirred solution of (3S.5R)- 3,5-dimethyl-piperazine-i-carboxylic acid tert-butyl ester (500 mg, 2.34 mmol) and TEA (0.49 ml, 3.51 mmol) in DCM (20 ml). The mixture was stirred at room temperature overnight, then the solvent was evaporated and the residue was partitioned between Et2O and 5% citric acid. The organic phase was dried over Na2SO4 and evaporated in vacuo to give 545 mg of (3S,5R)-4-acetyl-3,5-dimethyl- piperazine-1-carboxylic acid tert-butyl ester as a colourless oil. Y= 90%, 129779-30-2

The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DAC S.R.L.; WO2007/113249; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

234108-58-8, tert-Butyl 4-(2-aminoethyl)-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 95 1-[2-(Pyridazin-4-ylamino)-ethyl]-piperazin-2-one. 1-(2-Aminoethyl)-4-(tert-butyloxycarbonyl)-piperazin-2-one from EXAMPLE 92, Part A (1.0 g, 4.1 mmol) is treated with 3,4,5-trichloropyridazine (0.81 g, 4.1 mmol), triethylamine (0.57 ML, 4.1 mmol), THF (25 ML) and heated to 120 C. in a sealed tube for 3 hours.Upon cooling, the solution is diluted with ethyl acetate and washed with aqueous sodium bicarbonate (25 ML), water and dried over sodium sulfate.The organic layer is concentrated and chromatographed (5% methanol/methylene chloride) to give a mixture of isomers (0.8 g, 20 mmol).The mixture is dissolved in 0.5 M sodium methoxide in methanol (200 ML), treated with 10% Pd/C (0.5 g) and agitated under 50 PSI of hydrogen for 20 hours.The reaction mixture is filtered; the filtrate is concentrated to a residue which is chromatographed (NH4OH/H2O/MeOH/EtOAc, 1:1:2:90) to give crude 4-(tert-butyloxycarbonyl)-1-[2-(pyridazin-4-ylamino)-ethyl]-piperazin-2-one.This material is dissolved in a minimal amount of THF and treated with a saturated solution of HCl in ethyl acetate (50 ML).The solution is stirred at ambient temperature for 2 h and diluted with diethyl ether (50 ML).The precipitated title compoundcompound is collected and air dried (0.5 g, 1.7 mmol). MS m/z: 367, [M+1]+; 1H NMR (CD3OD, 300 MHz) delta8.8 (d, 1H), 8.5 (s, 1H), 7.4 (d, 1H), 4.1 (s, 2H), 3.5-3.8 (m, 8H).

234108-58-8, As the paragraph descriping shows that 234108-58-8 is playing an increasingly important role.

Reference£º
Patent; AVENTIS PHARMACEUTICALS INC.; US2004/102450; (2004); A1;,
Piperazine – Wikipedia
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

A modified procedure of Mahesh et al, Pharmazie, 2005, 60, 6, 411-414, was used. After cooling a stirred solution of N-methylpiperazine (50 mmol, 5.55 ml) in 100 ml acetone to 0 C, 10 ml of an aqueous 25 % NaOH-solution and l-bromo-3-chloropropane (50 mmol, 7.87 g = 4.92 ml) were added cautiously. The reaction was stirred at RT for 24 hours. After concentrating the mixture under reduced pressure, the residue was diluted with water and extracted with dichloromethane. The collected organic phases were dried over Na2S04, filtered and concentrated. The residue was diluted with ethanol and after adding 2.3 M ethanolic HC1 l-(3-chloropropyl)-4-methylpiperazin-dihydrochloride crystallized as white crystals(12.5 mmol, 25 %). Mp = 257 C. ]H NMR (300 MHz, DMSO) 3.74 (t; 2H; 3J = 6.4 Hz; NCH7CH7CH7CI); 3.37 (m; 12H: NCH7CH7CH7Cl+4xpiperazin-CH7+2x H); 2.81 (s; 3H; CH3); 2.19 (d; 2H; J = 6.8 Hz; NCH2CH2CH2CI).

109-01-3, As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Patent; JOHANNES GUTENBERG-UNIVERSITAeT MAINZ; DANNHARDT, Gerd; KRAMB, Jan-Peter; PLUTIZKI, Stanislav; WO2011/73092; (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.1403898-64-5,(2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation 46: (2R,5R) -4-(2,4-Di methoxy-benzyl)-5-hydroxymethyl-2-methyl-pi perazi ne1-carboxylic acid tert-butyl ester To an ice-cooled solution of (2R ,5R)-5-hydroxymethyl-2-methyl-piperazine- 1 -carboxylic acid tert-butyl ester (10.0 g, 43.5 mmol) in DOE (70 mL) were added 2,4-dimethoxy-benzaldehyde (11.1 g, 66.6 mmol) and sodium triacetoxyborohydride(11.1 g, 52.2 mmol) in small portions. Thereaction mixture was stirred at room temperature overnight. Saturated aqueous NaHCO3 was added and the product was extracted with DCM. The organic phase was dried and evaporated. Chromatography on silica gel, eluting with petrol – EtOAc 0-50% gave the title compound (16.3 g, 99%). 1297-012-1 MS: [M+H] = 381., 1403898-64-5

The synthetic route of 1403898-64-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; PAGE, Lee William; BUCK, Ildiko Maria; DAY, James Edward Harvey; HOWARD, Steven; SAXTY, Gordon; MURRAY, Christopher William; HOPKINS, Anna; WO2014/60767; (2014); 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.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of compound 7, 8, or 9 (1 equiv) in 1-butanol was added compounds 12(1.1 equiv) and p-toluenesulfonic acid (1 equiv). The mixture was placed in a pressure flask, and heated to 100C for 15h. The reaction mixture was quenched by saturated Na2CO3 aqueous solution, and then was extracted with DCM and the organic phase was washed with water, dried over anhydrous Na2SO4. The combined organic layer was concentrated under reduced pressure and was further purified by flash column chromatography using dichloromethane/methanol as eluent to afford product H1-H14, Y1-Y14, or L1-L14 as a pale yellow solid., 115619-01-7

As the paragraph descriping shows that 115619-01-7 is playing an increasingly important role.

Reference£º
Article; Hou, Yunlei; Zhu, Liangyu; Li, Zhiwei; Shen, Qi; Xu, Qiaoling; Li, Wei; Liu, Yajing; Gong, Ping; European Journal of Medicinal Chemistry; vol. 163; (2019); p. 690 – 709;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

Triethylamine (190mul, 1.37mmol) was added to a solution of commercially available (S)-(+)-2-methylpiperazine (125mg, 1.25mmol) in CH2Cl2 (7mL) at 0C and stirred for 5min. p-Toluenesulfonyl chloride (238mg, 1.25mmol) was then added and the mixture was stirred for 1h at 0C before being allowed to warm to room temperature and stirred for a further 4h. Water was then added and the aqueous layer was separated and extracted with CH2Cl2, before being washed sequentially with 1M HCl (50mL), water (50mL), saturated aqueous NaHCO3 solution (50mL) and saturated aqueous sodium chloride solution (50mL). The organic layer was separated, dried (Na2SO4), filtered and concentrated in vacuo to afford tosyl piperazine, (3S)-3-methyl-1-[(4-methylbenzene)sulfonyl]piperazine (310mg, 97%) as a white solid. The product could be used without further purification; mp 138.5-141C (acetone); [alpha]23D=+38.9[alpha]D23=+38.9 (c 0.93, CHCl3); numax (ATR)/cm-1 3352, 2971, 2922, 2863, 2821, 1605, 1452, 1325, 1165, 1133, 1121, 997, 914, 861, 811, 754s, 655; deltaH (500MHz, DMSO-d6) 7.61-7.59 (2H, m, 2¡ÁArH), 7.47-7.44 (2H, m, 2¡ÁArH), 3.41-3.37 (2H, m, CH2NTs), 2.85 (1H, dt, J 12.1 and 2.8, CH2NTs), 2.68-2.60 (2H, m, 3-H and CHHN(H)), 2.41 (3H, s, ArCH3), 2.06 (1H, td, J 11.3 and 3.1, CHHN(H)), 1.70 (1H, t, J 10.8, CHHN(H)), 0.90 (3H, d, J 6.4, 3-(CH3)); deltaC (126MHz, DMSO-d6) 143.4, 131.9, 129.7, 127.5, 52.3, 49.5, 45.9, 44.3, 20.9, 18.8; m/z (CI+) 255 (MH+, 100%), 99 (M+ -Ts, 10); HRMS (CI+) MH+ calculated for C12H19N2O2S 255.1167, observed 255.1164.

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference£º
Article; Armstrong, Alan; Pullin, Robert D. C.; Jenner, Chloe R.; Foo, Klement; White, Andrew J. P.; Scutt, James N.; Tetrahedron Asymmetry; vol. 25; 1; (2014); p. 74 – 86;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics