Month: October 2020

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, A mixture of 1-methylpiperazin-2-one (183 g, 1.6 mol) and diethyl ethoxymethylenemalonate (346 g, 1.6 mol) in toluene (12 L) was heated at 100 ¡ãC overnight. The resultant mixture was concentrated under vacuum. The residue was dissolved in anhydrous THF (8 L), brought to reflux under an atmosphere of nitrogen, and treated with a solution of lithium bis (trimethylsilyl)amide in THF (1 M, 1.05 eq). The reaction mixture was allowed to cool to room temperature and concentrated under vacuum. The residue was partitioned between methylene chloride and dilute aqueous HCI. The organic extract was washed with brine, dried over anhydrous magnesium sulfate, filtered, and concentrated under vacuum. The residue was triturated with ethyl acetate, cooled to -20 ¡ãC, and the solid precipitated was filtered to provide the title compound. 1H NMR (400 MHz, DMSO-d6) 8 8.50 (s, 1H), 7.33 (s, 1H), 4.18 (q, J = 7.1 Hz, 2H), 4.11 (t, J = 5.5 Hz, 2H), 3.59 (t, J = 5.5 Hz, 2H), 2.92 (s, 3H), 1.24 (t, J = 7.1 Hz, 3H). ES MS M+l = 239

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK & CO., INC.; WO2005/110414; (2005); A2;,
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.

A mixture of (4-chloro-[1,3,5]triazin-2-yl)-methyl-amine (290 mg, 2.00 mmol), Nal (28 mg)and 4-(4-ethylpiperazin-1-yl)-aniline (410 mg, 2.0 mmol) in EtOH (20 ml) and N-ethyl-diisopropyl amine (350 ul, 2.0 mmol) is heated to 80C for 3 h under a nitrogen atmosphere.The reaction mixture is cooled to RT, concentrated partially in vacuo and diluted with hexaneat 0 C. The precipitate is filtered off, washed with Et2O and re-dissolved in EE and water.The separated off aqueous phase is extracted twice with EE, the organic layer washed withwater and brine, dried (Na2SO4) and concentrated, yielding the title compound: ESI-MS: 314[MH]*; TLC: Rf = 0.10 (DCM/MeOH 9:1).

115619-01-7, 115619-01-7 4-(4-Ethylpiperazin-1-yl)phenylamine 936738, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; IRM LLC; WO2006/420; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

192130-34-0, General procedure: A suspension oftert-butyl 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-formyl-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl)benzoate5(1 eq.), the corresponding amine (2 eq.) and acetic acid (2 – 5 eq.) in DCE (2 ml) was stirred at RT for 30 min.To this suspension was added sodium triacetoxyborohydride (5 eq.).The resulted mixture was stirred at RT for 18 – 72 hrs.The reaction mixture was diluted with 5 ml of saturated sodium carbonate and extracted with DCM (3 x 10 ml).The combined organic layers were dried over sodium sulfate, filtered and concentratedinvacuo.The crude product was purified by Biotage flash chromatography or was used directly in the next step without further purification.

192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Chen, Yan; Sit, Sing-Yuen; Chen, Jie; Swidorski, Jacob J.; Liu, Zheng; Sin, Ny; Venables, Brian L.; Parker, Dawn D.; Nowicka-Sans, Beata; Lin, Zeyu; Li, Zhufang; Terry, Brian J.; Protack, Tricia; Rahematpura, Sandhya; Hanumegowda, Umesh; Jenkins, Susan; Krystal, Mark; Dicker, Ira D.; Meanwell, Nicholas A.; Regueiro-Ren, Alicia; Bioorganic and Medicinal Chemistry Letters; vol. 28; 9; (2018); p. 1550 – 1557;,
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.889958-14-9,1-Boc-2-oxopiperazine,as a common compound, the synthetic route is as follows.,889958-14-9

Methyl 4-(t-Butoxycarbonyl)-2-oxo-3-(4-benzyloxybenzyl)-1-piperazineacetate (4a) To a solution of dry diisopropylamine (0.31 ml, 2.2 mmole) in 2 ml of dry THF at 0 C. under argon was added dropwise via syringe a hexane solution of n-butyllithium (0.9 ml, 2.2 mmole). After about 1/2 hour, a solution of t-boc piperazinone (2) (0.200 g, 1.00 mmole) in 5 ml of THF was added dropwise via syringe. The resulting solution was allowed to metallate at 0 C. for 3 hours after which a solution of 4-benzyloxybenzyl chloride (0.256 g, 1.1 mmole) in 2 ml of dry THF was added and the resulting solution stirred at 0 C. for one hour, allowed to warm to room temperature and stirred overnight. Methyl alpha-bromoacetate (0.095 ml, 1.1 mmole) was added to the solution via syringe and the solution stirred overnight at room temperature and quenched into ethyl ether/water. The aqueous phase was extracted twice with ether and the combined ethereal extracts washed with saturated sodium chloride solution and dried over Na2 SO4. The solvent was evaporated and the resulting yellow oil chromatographed with 20% ethylacetate/chloroform to yield 4a, as an oil, which crystallized upon standing. M.p. 84-87 C.

889958-14-9 1-Boc-2-oxopiperazine 21868412, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Richardson-Merrell Inc.; US4341698; (1982); A;,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Step 1: 2-Methylpiperazine (5.03 g) was dissolved in dichloromethane (200 mL) and a solution of di-tert-butyl-dicarbonate (10.96 g) in dichloromethane (100 mL) was added over 2.5 hours. The reaction was stirred at room temperature for 24 hours and concentrated to dryness giving 1-BOC-3-methylpiperazine. Yield=100percent, 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Millennium Pharmaceuticals, Inc.; US2003/153556; (2003); 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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

40 mg of compound III and 56 mg of cyclopropylpiperazine, 2 drops of glacial acetic acid were added to 5 ml of anhydrous methanol, stirred, heated to 60 C, and reacted for 4 hours.Then, 50 mg of sodium cyanoborohydride (NaBH3CN) was added and reacted at room temperature for 12 hours.TLC monitoring, antiAfter completion, the solvent was evaporated, the reaction was poured into 100 mL of water, and extracted with ethyl acetate (20 mL¡Á3),The phases were washed with 5% NaHCO 3 (20 mL¡Á3), saturated brine (20 mL¡Á3), and dried over anhydrous magnesium sulfate.Filtration, removal of ethyl acetate under reduced pressure, followed by column chromatography V (dichloromethane):V (methanol) = 20:1 gave white solid compound C7 8 mg., 20327-23-5

As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference£º
Patent; Southern Medical University; Chen Jianjun; Cheng Binbin; (23 pag.)CN109503546; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78551-60-7,tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Sodium hydride (80 mg, 2.0 mmol, 60% in mineral oil) was added to a solution of 4-tert-butyloxycarbonyl-piperazin-2-one (200 mg, 1.0 mmol) in dimethylformamide (5.0 mL) at 0 C. The reaction was stirred at 0 C. for 0.5 h. To this mixture was added benzyl bromide (300 uL, 2.5 mmol) and the reaction was stirred for 2 h at room temperature. The reaction mixture was quenched with a dilute aqueous solution of sodium bicarbonate and extracted with methylene chloride. The organic extracts were washed with brine and dried over anhydrous sodium sulfate. Purification of the crude residue by chromatography over silica gel using 30% ethyl acetate in hexane gave 4-tert-butyloxycarbonyl-2-benzyl-piperazin-2-one (174 mg, 60% yield). [0350] Hydrochloric acid (0.25 mL, 1.00 mmol, 4 M in 1,4-dioxane) was added to a solution of 4-tert-butyloxycarbonyl-2-benzyl-piperazin-2-one (174 mg, 0.60 mmol) in 1,4-dioxane (1.0 mL). The mixture was stirred overnight. The reaction was concentrated to give 2-benzyl-piperazin-2-one hydrochloride as an off-white solid (130 mg, 97% yield). [0351] 4,5-Bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazole-1-carbonyl chloride (example 3) was reacted with 2-benzyl-piperazin-2-one hydrochloride using the procedure as described in example 5 to give 4-[4,5-bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazole-carbonyl]-1-benzyl-piperazin-2-one. It was then dissolved in dilute hydrochloric acid (0.5 N, 1 mL) and lyophilized to give 4-[4,5-bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazole-carbonyl]-1-benzyl-piperazin-2-one hydrochloride as an off-white powder (65 mg, 89% yield). LR-MS (APCI): 695.6 [(M+H)+].

The synthetic route of 78551-60-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Haley, Gregory Jay; Kong, Norman; Liu, Emily Aijun; Simonsen, Klaus B.; Vu, Binh Thanh; Webber, Stephen Evan; US2004/259884; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6,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.

Example 108 (E)-4-(3-(3,3,6,6-tetramethylcyclohex-1-enyl)acryloyl) piperazine-1 -carboxamideExample 108a. Tert-Butyl 4-carbamoylpiperazine-1-carboxylate To a solution of terf-butyl piperazine-1 -carboxylate (5.0 g, 26.8 mmol) in acetic acid (15 mL) and water (25 mL) was added a solution of potassium cyanate (11.25 g, 138.9 mmol) in water (25 mL) dropwise. After addition the mixture was stirred at rt for 4h, during which time a solid precipitated. The solid was collected by filtration, re-dissolved in dichloromethane (20 mL), dried oversodium sulfate, and filtered. The filtrate was concentrated to give the title compound as a white solid (3.3 g, yield: 53%), which was used in the next step without further purification. 1H NMR (400 MHz, DMSO-d6) delta 6.04 (s, 2H), 3.26 (s, 8H), 1.41 (s, 9H)

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

Reference£º
Patent; BIKAM PHARMACEUTICALS, INC.; GARVEY, David, S.; LAROSA, Gregory, J.; GREENWOOD, Jeremy, Robert; BREWER, Mark, L.; QUACH, Tan; COTE, Jamie, B.; BERMAN, Judd; WO2010/147653; (2010); 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.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,154590-35-9

To a solution of 4-(4-Amino-2-fluoro-phenyl)-piperazine-1 -carboxylic acid te/t-butyl ester (0.50 g, 1.7 mmol) and (0.38 g, 1.9 mmol) in CH2CI2 (30 ml_) was added 1 -hydroxybenzotriazole hydrate (0.27 g, 2.0 mmol), and 1 -[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (0.38 g, 2.0 mmol). After stirring at room temperature for 18 h, the reaction was diluted with 1 N NaOH (50 ml_) and extracted with CH2CI2 (3×50 ml_). The organic extracts were combined, dried (Na2SO4), and concentrated. Chromatography of the resulting residue (SiO2: EtOAc/hexanes) yielded 4-{4- [(biphenyl-2-carbonyl)-amino]-2-fluoro-phenyl}-piperazine-1 -carboxylic acid tert- butyl ester, which was further dissolved in MeOH (20 ml_) and 4N HCI in dioxanes. After stirring for 5 h, the reaction mixture was concentrated down, neutralized with 1 N NaOH, and extracted with EtOAc (3x75ml_). The orgranic extracts were combined, dried (Na2SO4), and the solvent was evaporated under reduced pressure to yield the title compound.MS (ESI): mass calcd. for 023Hz2FN3O, 375.17; m/z found, 376.3 [IvRH]+.

The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA, N.V.; WO2009/6185; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

655225-01-7, tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

655225-01-7, Example 63B; tert-butyl 4-(2-(3,3-bis(4-fluorophenyl)-2-oxopyrrolidin-l-yl)ethyl)piperazine-l- carboxylate; To a solution of 3,3-bis(4-fluorophenyl)pyrrolidin-2-one (Example 58B, 1.37 g, 5.00 mmol) in tetrahydrofuran (30 mL) was added potassium t-butoxide (1.0 M in tetrahydrofuran) (7.5 mL, 7.5 mmol) followed by the product from Example 63A (1.47 g, 5.00 mmol). The reaction mixture was heated at 75 0C for 18 hours. The reaction was concentrated, diluted with ethyl acetate, washed with water and brine, dried with MgSO4, filtered and concentrated. The residue was purified with silica gel chromatography eluting with 3percent methanol/dichloromethane to give the title compound. MS (DCI) m/z 486.3(M+H)+.

655225-01-7 tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate 15946441, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ABBOTT LABORATORIES; BHATIA, Pramila, A.; DOHERTY, George, A.; DRIZIN, Irene; MACK, Helmut; PERNER, Richard, J.; STEWART, Andrew, O.; ZHANG, Qing Wei; WO2010/39947; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics