Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of compound 5a-b (2 mmol) in dry DCM (10 mL) was added K2CO3 (1.1 equiv, 2.2 mmol, 304 mg). The mixture was cooled with a bath of ice/water, and then the appropriate N-substituted piperazine (2 equiv, 4 mmol), dissolved in DCM (2 mL), was added slowly over 30 min. The mixture was then stirred at room temperature for two hours, diluted with DCM (10 mL), washed with water (10 mL) and then with brine (10 mL). The organic layer was dried (Na2SO4), filtered and concentrated in vacuo to give a brown residue that was purified by column chromatography to furnish the derivatives 6a-aq.

115761-79-0, As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference：
Article; Romagnoli, Romeo; Baraldi, Pier Giovanni; Carrion, Maria Dora; Cara, Carlota Lopez; Cruz-Lopez, Olga; Salvador, Maria Kimatrai; Preti, Delia; Tabrizi, Mojgan Aghazadeh; Shryock, John C.; Moorman, Allan R.; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Bioorganic and Medicinal Chemistry; vol. 20; 2; (2012); p. 996 – 1007;,
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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

13484-40-7, A mixture of 1.0 g (6.9 mmol) of the compound from Example 7A and 1.1 g (7.6 mmol) 1-(2-methoxyethyl)piperazine in 10 ml water is stirred at 100 C. for 2 h. A further 0.9 g (6.2 mmol) 1-(2-methoxyethyl)piperazine is added and the reaction mixture is stirred further at 100 C. for 16 h. After concentration in vacuo, the residue is stirred in acetonitrile. The solid which has precipitated out is filtered off, washed first with ethanol and then with diethyl ether and dried in vacuo.Yield: 0.8 g (42% of th.)LC-MS (Method 8): Rt=0.22 min; MS (ESIpos): m/z=253 [M+H]+;1H-NMR (400 MHz, DMSO-d6): delta=7.93 (s, 1H), 7.64 (s, 1H), 5.91 (s, 1H), 4.14 (s, 2H), 3.50-3.40 (m, 6H), 3.24 (s, 3H), 2.47-2.39 (m, 4H).

13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BAYER SCHERING PHARMA AKTIENGESELLSCHAFT; US2010/305085; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-71-6, (q) tert-butyl4-(2-bromoacetyl)piperazine-1-carboxylate (6q) Under inert atmosphere and at -78C, bromoacetylbromide (53.7 mmol, 1 eq.) was slowly added to a solution of Boc-piperazine(53.7 mmol, 1 eq.) and TEA (59.1 mmol, 1.1 eq.) in DCM (150 ml). The reactionmixture was stirred at -78C for 3h, diluted with DCM (75 ml) and washed withwater. The recovered organic layer was dried over magnesium sulfate and thesolvent was evaporated under vacuum. The obtained crude product was furthertriturated with diethyl ether, filtered and dried under vacuum to conduct tothe desired acetylated compound. CnHi 9BrN 20 3; yield 78%; white solid; m.p.243-244 C; M = 307.18 g/mol; IR (KBr): v = 2965 (m), 1689 (s), 1632 (s), 1417(s), 1246 (s), 1167 (s), 1023 (m); cm – ; NMR (250 MHz, CDCI 3) delta 3.87 (s, 2H), 3.61-3.57 (m, 2H), 3.55-3.47 (m,4H), 3.46- 3.41 (m, 2H), 1.46 (s, 9H); C NMR (63 MHz, CDCI 3) delta 165.5 (C q), 154.5 (C q), 80.5 (C q), 46.6 (2CH2), 40.9 (2CH 2), 28.4 (3CH 3), 25.7 (CH 2);

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

Reference：
Patent; ASTON UNIVERSITY; GRIFFIN, Martin; RATHBONE, Daniel; BADARAU, Leonas Eduard; WO2014/57266; (2014); A1;,
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

A solution of 4-(2,4-dichloro-phenyl)-1H-pyrazole-3-carboxylic acid (70 mg; 0.27 mmol), 4-(4-methyl-piperazin- 1-yl)-benzylamine (62 mg; 0.3 mmol), EDAC (63 mg; 0.33 mmol) and HOBt (45 mg; 0.33 mmol) in 5 ml of DMF was stirred at room temperature for 48 hours. The reaction was evaporated and the residue partitioned between ethyl acetate and brine. The ethyl acetate layer was separated, dried (MgSO4), filtered, evaporated then dried further under vacuum to give 34 mg of 4-(2,4-dichloro-phenyl)-1H-pyrazole-3-carboxylic acid 4-(4- methyl-piperazin-1-yl)-benzylamide. (LC/MS: Rt 2.42 [M+H]+444)., 216144-45-5

As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference：
Patent; ASTEX THERAPEUTICS LIMITED; WO2006/77425; (2006); A1;,
Piperazine – Wikipedia
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

Example 6 (Z)-5-(3-chloro-2-(4-cyclopentylpiperazin-1-yl)-5 (trifluoromethyl)benzylidene)thiazolidine-2,4-dione hydrochlorideA 40 mL vial was charged with a magnetic stir bar, 3-chloro-2-fluoro-5-(trifluoromethyl)benzaldehyde (0.134 ml, 1.10 mmol), acetonitrile (2.76 ml), 1-cyclopentylpiperazine (0.213 g, 1.38 mmol), and K2CO3 (0.229 g, 1.66 mmol). The vial was heated to 70 C. with stiffing for 2 h. The vessel was then cooled to rt and the mixture was diluted with DCM and filtered. The filtrate was conc. in vacuo to afford the substituted aldehyde which was dissolved in EtOH (2.76 ml). Thiazolidine-2,4-dione (0.155 g, 1.32 mmol) and piperidine (9.40 mg, 0.11 mmol) were then added and the mixture was heated to reflux for 4 h before being allowed to cool to rt. The mixture was then conc. in vacuo to afford the product which was dissolved in DMSO (2 mL) and purified via reverse phase HPLC to afford fractions that were conc. in vacuo, suspended in methanol (5 mL) and 1N HCl in diethyl ether (2 mL). This mixture was conc. in vacuo to afford (Z)-5-(3-chloro-2-(4-cyclopentylpiperazin-1-yl)-5-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione hydrochloride (0.215 g, 39.3%). 1H NMR (300 MHz, DMSO-D6) delta ppm 12.78 (s, 1H) 7.96 (s, 1H) 7.83 (s, 1H) 7.63 (s, 1H) 3.77-3.50 (m, 5H) 3.30-3.22 (m, 2H) 3.08-2.99 (m, 2H) 2.03-1.99 (m, 2H) 1.84-1.61 (m, 4H) 1.60-1.50 (m, 2H); m/z 461.

21043-40-3, As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; US2011/218182; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1403898-64-5, (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Finely ground potassium iodide (7.5 g, 45.26 mmol) was added to a mixture of (2R,5R)-5- hydroxymethyl-2-methyl-piperazine- 1 -carboxylic acid teit-butyl ester (5.7 g, 24.89 mmol), 2- chloro- 1 -[6-(4-fluorobenzyl)-3, 3-dimethyl-2, 3-dihydro-pyrrolo[3,2-b]pyridin- 1 -yl]-ethanone hydrochloride (8.35 g, 22.63 mmol) potassium carbonate (12.5 g, 90.51 mmol) andacetonitrile (100 mL) under nitrogen. The mixture was stirred at 20 C overnight. The mixture was partitioned between water (300 mL) and EtOAc (300 mL) and the organic phase was dried and evaporated in vacuo to give the title compound (12.14 g). MS: [M+H] = 527., 1403898-64-5

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

Reference：
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; PAGE, Lee William; MILLEMAGGI, Alessia; HOWARD, Steven; SAXTY, Gordon; HEIGHTMAN, Thomas Daniel; WO2014/60768; (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.1284243-44-2,tert-Butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Hydrogen chloride (4 N in 1 ,4-dioxane) (4 mL, 32 mmol) was added and the mixture was stirred at room temperature for several hours. The solvent was evaporated to give the title compound (0.135 g, quantitative) as a white solid. 1H NMR (400 MHz, DMSO-Qf6) delta ppm 9.79 (br. s., 1 H) 7.34 – 7.41 (m, 2 H) 7.25 – 7.34 (m, 2 H) 3.82 – 3.92 (m, 4 H) 3.53 (d, 2 H)., 1284243-44-2

As the paragraph descriping shows that 1284243-44-2 is playing an increasingly important role.

Reference：
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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

859518-35-7, tert-Butyl 3-cyanopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,859518-35-7

To a solution of ten-butyl 3-cyanopiperazine-1-carboxylate (21.1 g, 0.1mol) and aqueous formaldehyde (24 g. 37% in water) in THF was added sodiumcyanoborohydride (315 g, 0.5 rnol) in small portions. The reaction mixture was agedat ambient temperature overnight then diluted with water and extracted with ethylacetate. The organic phase was washed with saturated aqueous sodium chloride,dried over anhydrous sodium sulfate. filtered, and concentrated under vacuum. Thecrude product was purified by column chromatography to provide the title compound.1H NMR (400MHz, MeOD) o 4.23-4.18 (m, 1H), 4.01-3.97 (br, 1H), 3.92-3.90 (br,1 H), 2.92-2.89 (br, 1 H). 2.88-2.87 (br, 1 H), 2.65-2.62 (m, 1 H), 2.378 (s, 3H), 2.36-2.33 (m, 1H), 1.47 (s, 9H).

859518-35-7 tert-Butyl 3-cyanopiperazine-1-carboxylate 53487922, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ORTHO-CLINICAL DIAGNOSTICS, INC; JANSSEN PHARMACEUTICA NV; HRYHORENKO, Eric; SANKARAN, Banumathi; DECORY, Thomas, R.; TUBBS, Theresa; COLT, Linda; REMMERIE, Bart, M.; SALTER, Rhys; DONAHUE, Matthew, Garrett; GONG, Yong; WO2014/31656; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5271-27-2, 1-Methyl-3-phenylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5271-27-2, 1 -Methyl-3-phenylpiperazine (123.2 g; 0.70 mol) was dissolved in 500 dichloromethane. Triethylamine (30 ml; ca 0.2 mol) was added. A solution of ethyl chlorooxalate (107 g; 0.78 mol) in dichloromethane was slowly added under cooling. At 2/3 of the total addition a thick suspension was formed. Even after addition of more solvent, stirring remained difficult. The mixture was quenched with 10percent sodium carbonate. The organic layer is washed again with carbonate, dried and evaporated to an orange oil (191.2 g; 0.69 mol; 99 percent). Crystallisation with seeding proved difficult. Deep evaporation and storage as oil.TLC: very pure, a small amount of coloured polar material on baseline. No trace of the dioxamide (prepared from oxalylchloride and piperazine). GC: 18.0/18.2 min, 0.36 areapercent of 3.8 min impurity. A small sample (20 g) was stirred with water to induce crystallisation. mp ca 45 °C. The main bulk of the oil solidified after a few days of standing. Melting was needed before use.

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

Reference：
Patent; N.V. ORGANON; WO2007/144409; (2007); 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.509073-62-5,tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,509073-62-5

Step b – terf-butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate; A solution of tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate (1.0Og, 3.00mmol) in MeOH (60ml) was hydrogenated at 2O0C at atmospheric pressure using an H-Cube (flow rate at 1 ml/min and full hydrogen mode) using a Pd/C cartridge. The solvent was removed in vacuo Xo afford te/f-butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate (0.85g, 2.79mmol, 93%) as a white solid. 1H NMR (CDCI3) delta 1.41 (9H, s), 3.38 (4H, m), 3.53 (4H, m), 4.07 (2H, br. s), 6.55 (2H, d), 7.17 (2H, d). LCMS (2) Rt: 2.14min; m/z (ES+) 306.

The synthetic route of 509073-62-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SAREUM LIMITED; WO2008/139161; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics