Category: piperazines

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.

To a solution of 2-methylpiperazine (2.2 g) in tetrahydrofuran (15 ml) was added di-tert-butyl dicarbonate (4.0 g) slowly under ice-cooling, and the mixture was stirred at room temperature for 3.5 hours. Then the reaction mixture was diluted with ethyl acetate (20 ml), washed successively with water and brine, and dried over magnesium sulfate. The solvent was evaporated to give the title compound as a colorless oil. The obtained compound was used for the next step without further purification. [00318] 1H-NMR (300 MHz, CDCl3) delta 1.04 (d, J=5 Hz, 3H), 1.45 (s, 9H), 2.40 (br, 1H), 2.65-2.86 (m, 4H), 2.88-3.08 (m, 1H), 3.75-4.15(m, 2H).

109-07-9, As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; Fujisawa Pharmaceutical Co., Ltd.; US6825200; (2004); B1;,
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1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound (II) (20.0 g, 35.0 mmol)Dissolved in 300mL of dichloromethane (DCM),Add sequentially at room temperature3-nitro-4-fluorobenzenesulfonamide (8.5 g, 38.5 mmol),4-dimethylaminopyridine (DMAP) (6.4 g, 52.5 mmol),1-Ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC.HCL) (10.1 g, 52.5 mmol).The reaction was stirred at a temperature of 20 to 30 C for 16 hours.After the reaction was completed, it was washed once by adding 100 mL of a 5% acetic acid aqueous solution.Then wash it again with 100 mL of water.The organic phase is dried with 20 g of sodium sulfate.Filter, spin dry,The fluorine-containing compound (III) solid was 26.1 g, and the yield was 96.3%.Used directly for the next step.

1235865-77-6, The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chongqing San Sheng Industrial Co., Ltd.; Peng Lei; Huang Xiongjiu; He Wei; Tang Lichang; Liu Ling; Chen Zhenming; (12 pag.)CN109438441; (2019); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

76003-29-7, 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)+].

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; Haley, Gregory Jay; Kong, Norman; Liu, Emily Aijun; Simonsen, Klaus B.; Vu, Binh Thanh; Webber, Stephen Evan; US2004/259884; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.6531-38-0,2,2′-(Piperazine-1,4-diyl)diethanamine,as a common compound, the synthetic route is as follows.

To Intermediate 50.2 (500 mg, 2 91 mmol, 1 00 equiv) m dichloromethane (10 mL) was added tnethylamme (1 46 g, 0 01 mmol, 2 00 equiv) and 4-(benzyloxy)benzene-l-sulfonyl chlo?de (2 0 g, 0 01 mmol, 240 equiv) and the resulting solution was stirred for 2 h at room temperature The reaction was diluted with dichloromethane, washed with 3×10 mL of water, dried over sodium sulfate then filtered and concentrated under vacuum to afford 0 9 g (47%) of Intermediate 50 3 as a yellow solid., 6531-38-0

The synthetic route of 6531-38-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARDELYX, INC.; CHARMOT, Dominique; JACOBS, Jeffrey, W.; LEADBETTER, Michael, Robert; NAVRE, Marc; CARRERAS, Chris; BELL, Noah; WO2010/78449; (2010); A2;,
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182618-86-6, 1-Boc-4-(4-Nitrophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of 1a (5 g, 22.5 mmol) in 95% ethanol (100 mL) wasadded goethite (FeO(OH))/C (1.0 g) at room temperature. And a solution of 80% hydrazine hydrate (25 mL, 400 mmol) in 95% ethanol (50 mL) was added dropwise to the mixture at 0 C. The reaction mixture was stirred at 80 C for 4 h. The solvent was removed in vacuo to give 2a (3.8 g, yield 74.5%). MS m/z: 278.2 [M+H]+.

182618-86-6, As the paragraph descriping shows that 182618-86-6 is playing an increasingly important role.

Reference£º
Article; Bao, Jiyin; Liu, Haichun; Zhi, Yanle; Yang, Wenqianzi; Zhang, Jiawei; Lu, Tao; Wang, Yue; Lu, Shuai; Bioorganic Chemistry; vol. 94; (2020);,
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59878-57-8,59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The synthetic route is: Piperazine cyclopropyl ketone (1.1g, 0.0071mol)Soluble in 25ml anhydrous acetonitrile,Add potassium carbonate (4.0g, 0.029mol), cool to 0 , nitrogen protection,Stir vigorously. Compound 5 (2.1g, 0.0066mol),Dissolve with 20ml of anhydrous acetonitrile and slowly add dropwiseAfter the addition, the temperature was raised to room temperature, a small amount of DMAP (0.5g, 0.0041mol) was added, and the reaction was carried out for 6h.Concentrate under reduced pressure, add 40ml of water, adjust the pH to 8 with sodium bicarbonate, extract with ethyl acetate, concentrate under reduced pressure to remove the solvent, recrystallize with ethyl acetate, filter to obtain light red solid, decolorize with a small amount of activated carbon, filter and concentrate It was dried to obtain a white solid (2.8g, yield 93%).

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Southeast University; Cai Jin; Ren Jinghui; Hu Xinyi; Wei Lili; Yu Ping; Huang Mingqi; (8 pag.)CN110790710; (2020); A;,
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694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

694499-26-8, Example 16: 6-[[6-(Amino)-4-pyrimidinyl]oxy]-N-[4-[(4-methyl-1 -piperazinyl)methyl]-3- (trifiuoromethyl)phenyl]-1-naphthalenecarboxamide; A solution containing ~50% of propylphosphonic anhydride in lambda/,lambda/-dimethylformamide (Fluka; 700 mul_, -1.1 mmol) is added to a stirred mixture of 6-[(6-amino-4-pyrimidinyl)oxy]-1- naphthalenecarboxylic acid (200 mg, 0.71 mmol), 4-[(4-methyl-1- piperaziny.)methyl]benzeneamine (194 mg, 0.71 mmol) and triethylamine (812 mul_, 6 mmol) in 10 mL lambda/./V-dimethylformamide. After stirring for 24 hours at 5O0C1 the mixture is treated with a saturated aqueous sodium hydrogen carbonate and extracted with ethyl acetate. The combined extracts are dried (Na2SO4) and solvent is evaporated off under reduced pressure to give a residue, which is purified by column chromatography (SiO2; CH2CI2/MeOH/NH3(d 0.88) 90:9:1) and recrystallised from ethylacetate-hexane to afford the title compound as a pale-yellow solid, m.p.: 127-1300C.

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVARTIS AG; WO2008/125691; (2008); A2;,
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4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 4-bromobenzoic acid 1-12 at 0¡ãC (2 g, 9.94 mmol) in a mixture of MeC : DMF (4:1, 20 mL) were added HATU (4.53 g, 11.93 mmol) and 1-isopropylpiperazine (1.91 g, 14.92 mmol). The reaction mixture was allowed to stir for 30 minutes, and then diisopropylethylamine (3.85 g, 5.2 mL, 29.84 mmol) was added thereto. The resulting reaction mixture was stirred for 16 hours at room temperature. After completion of reaction, the reaction mixture was diluted with water and extracted with ethyl acetate (25 mL x 3) . The combined organic layer was washed with water and brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The obtained residue was purified by silica gel ‘(60-120 mesh size) column chromatography using 0-5 percent methanol in dichloromethane as eluent to give the desired product 1-13 (3.0 g, 97percent) as brown solid; LCMS: m/z 312.00 (M+l) .

4318-42-7, As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; KOUL, Summon; KURHADE, Suresh; BHOSALE, Sandeep; NAIK, Keshav; SALUNKHE, Videsh; MUNOT, Yogesh; BHUNIYA, Debnath; (284 pag.)WO2015/88045; (2015); A1;,
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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.

A mixture of Intermediate 41 (0.3g), (2S)-2-methylpiperazine (CAS No 74879-18-8) (0.1g) and TEA (0.12g) in methanol (20.OmL) is heated at 650C for 4 hours. The solvent is evaporated in vacuo. Purification of the residue by column chromatography on silica, eluting with DCM / methanol (95:5), affords the title compound as a white solid (0.26g, 73%). LCMS 362/364 [M+H]+, RT 2.24 mins (pH 5.8). 1H NMR 300 MHz (CDCI3) (delta ppm):8.15 (1 H, d), 7.60 (1 H, dd), 7.40 (1H, d), 4.85 (4H, m) 3.15 (2H, m), 2.95 (2H, m), 2.75(1 H, t), 1.95 (3H, d)., 74879-18-8

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

Reference£º
Patent; UCB PHARMA, S.A.; WO2008/74445; (2008); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: (S)-tert-butyl-2-methyl-4-phenylpiperazine-1-carboxylate To a solution of iodobenzene (2.08 g, 10.19 mmol) in toluene (60 mL) at rt was added (S)-tert-butyl-2-methylpiperazine-1-carboxylate (1.7 g, 8.49 mmol), Pd2(dba)3 (778 mg, 0.85 mmol), t-BuONa (2.44 g, 25.46 mmol), XantPhos (982 mg, 1.70 mmol) under nitrogen. The reaction mixture was stirred at 100 C. for 16 h, then cooled to rt and diluted with EtOAc (60 mL*3). The combined organic layers were washed with brine, dried over Na2SO4, filtered, concentrated, and purified by chromatography (silica, EtOAc/PE=1/10) to afford (S)-tert-butyl-2-methyl-4-phenylpiperazine-1-carboxylate (1.8 g, 6.5 mmol, 64%) as an oil. ESI-MS (EI+, m/z): 277.2 [M+H]+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); A1;,
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Piperazines – an overview | ScienceDirect Topics