Month: March 2021

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 17 4-({3-Chloro-4-[(1-ethyl-4,5-dimethyl-1H-imidazol-2-yl)sulfanyl]phenyl}amino)-7-[3-(4-ethyl-1-piperazinyl)propoxy]-6-methoxy-3-quinolinecarbonitrile To a stirred solution of 4-[3-chloro-4-(1-ethyl-4,5-dimethyl-1H-imidazol-2-ylsulfanyl)-phenylamino]-7-(3-chloro-propoxy)-6-methoxy-quinoline-3-carbonitrile (0.300 g, 0.539 mmol) in DMF (2 mL) was added 1-ethyl-piperazine (0.137 mL, 1.08 mmol) and NaI (0.008 g, 0.0539 mmol). The solution was heated to 100 C., maintaining the temperature overnight. The solution was cooled to room temperature and then diluted with brine (2 mL) and H2O (2 mL). The precipitate was collected via vacuum filtration and washed with H2O and Et2O to afford the product (0.290 g, 85%) as a solid, mp. 229-230 C.; 1H NMR (DMSO-d6) delta 0.93 (t, J=7.2 Hz, 3H), 1.04 (t, J=7.1 Hz, 3H), 1.85-1.95 (m, 2H), 2.07 (s, 3H), 2.15 (s, 3H), 2.22-2.43 (m, 12H), 3.86 (s, 3H), 3.90 (dd, J=7.1, 14.4 Hz, 2H), 4.14 (t, J=6.4 Hz, 2H), 6.58 (d, J=8.6 Hz, 1H), 7.06 (dd, J=2.3, 8.7 Hz, 1H), 7.29 (s, 1H), 7.30 (d, J=2.3 Hz, 1H), 7.61 (s, 1H), 8.45 (s, 1H), 9.46 (s, 1H); mass spectrum [(+) ESI], m/z 634/636 (M+H)., 5308-25-8

5308-25-8 1-Ethylpiperazine 79196, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Wyeth; US2009/264427; (2009); 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.113028-17-4,Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate,as a common compound, the synthetic route is as follows.

Ethyl-6-fluoro-1 -methyl-4-oxo-7-(1 -piperazinyl)-4H-(1 ,3)-thiazeto-[3,2-a]-quinoline-3- carboxylate (100 gms, 0.265 moles) was stirred in water (600 ml) at 25-30C. To this potassium hydroxide solution (50 gms of potassium hydroxide flakes is dissolved in 200 ml of water) was added and the reaction mass was heated to 80-85C. The contents were stirred for 1 hour and after completion of reaction, the reaction mass was cooled to 25-30C. The pH of the reaction mass was adjusted to 6.5-7.0 using 1:1 aqueous acetic acid solution. The contents were stirred at room temperature for 1 hour. The precipitated solid was filtered, washed with water (2 x 100 ml). The solid was slurried in methanol (300 ml) for 1 hour at 25-30C, filtered, washed with methanol (2 x 50 ml) and dried under vacuum at 70-75C to yield the title compound [90 gms, 97% yield, 96% HPLC purity].

113028-17-4, As the paragraph descriping shows that 113028-17-4 is playing an increasingly important role.

Reference£º
Patent; CIPLA LIMITED; PATHI, Srinivas Laxminarayan; RAO, Dharmaraj Ramachandra; KANKAN, Rajendra; CHINIMILLI, Venugopalarao; CURTIS, Philip Anthony; WO2012/1357; (2012); 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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

To a solution of (E)-methyl l-acetyl-3-(ethoxy(phenyl)methylene)-2-oxo- 2,3-dihydro-lH-pyrrolo[3,2-c]pyridine-6-carboxylate (40 mg, 0.109 mmol) in DMF (0.2 mL) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-l-yl)acetamide (28 mg, 0.109 mmol) at room temperature, and the reaction mixture was stirred at 110 C for 2h. The reaction mixture was cooled to RT, piperidine (0.2 mL) was added and stirred for 10 minutes at room temperature. The solvent was evaporated and the resulting residue was purified by silica gel column chromatography using 5% CH3OH in dichloromethane as eluent to afford (Z)-methyl 3- (((4-(N-methyl-2-(4-methylpiperazin-l-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxo- 2,3-dihydro-lH-pyrrolo[3,2-c]pyridine-6-carboxylate as yellow solid. MS (ES+): m/z 541.3 (MH+)., 262368-30-9

The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ANGION BIOMEDICA CORP.; PANICKER, Bijoy; MISHRA, Rama, K.; JUNG, Dawoon; OEHLEN, Lambertus, J.W.M.; LIM, Dong, Sung; WO2013/112959; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1001180-21-7, (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1001180-21-7, A 3000 L glass-lined reactor was evacuated and filled with nitrogen to normal pressure 3 times. Water (660.0 kg) was added into the reactor while maintaining the temperature in the range of 20-30 C. The stirrer was started, followed by the addition of potassium dihydrogen phosphate (9.2 kg), dipotassium phosphate (23.7 kg) and glucose (78.5 kg). The mixture was stirred until solid dissolved completely. Then 30.1 kg of this buffer mixture was discharged into a 50 L drum for future use. To the reactor was added (R)-tert-butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate (66.0 kg) and PEG400 (732.6 kg) and the mixture was heated to about 30-35 C. Maintaining the temperature at 30-35 C., a mixture of buffer solution (20.0 kg), KRED-101 (2.4 kg), GDH (3.4 kg) and NADP (2.2 kg) was added into the mixture. The mixture was then maintained at 32-37 C. for reaction while controlling the pH at 6.8-7.1. After about 6 h, the mixture was monitored by TLC and HPLC until ketone starting substrate was ?1.0%. During the reaction, potassium hydroxide solution (total 46.2 kg) and extra enzyme buffer solution prepared with purified water (5.0 kg), KRED-101 (0.24 kg), GDH (0.34 kg) and NADP (0.22 kg) were added. To a glass-lined reactor, isopropyl acetate (1148.6 kg) was added. The reaction mixture from the previous paragraph was added to the reactor in three portions. Each time, it was stirred for 15-20 min and held for at least 0.5 h before separation at 20-30 C. This extraction process was repeated three times. The organic phases were combined. At 20-30 C., the combined organic phases were washed with purified water (329.3 kg). It was stirred for 25-30 min and held for at least 30 min before separation. The organic phase was left in the reactor and the washing process was repeated. The organic phase was decolorized with active carbon (6.6 kg) and stirred for 1-1.5 h. The mixture was filtered via a Nutsche filter. The cake was washed with isopropyl acetate (57.5 kg). The filtrates were combined. The filtrate was then transferred into a thin film evaporator and concentrated at ?55 C. under reduced pressure until 500-600 L remained. The concentrated mixture was filtered and transferred into a glass-lined reactor, then concentrated at ?55 C. under reduced pressure until 50-60 L remained. The mixture was then heated to 50-55 C. and stirred at this temperature for 0.5-1.5 h under nitrogen. n-Heptane (277.2 kg) was added into the mixture at the rate of 20-30 kg/h while maintaining the temperature at 50-55 C. The mixture was then cooled to 20-30 C. at the rate of 5-10 C./h. The mixture was stirred at 20-30 C. for 1 h, then heated to 50-55 C. and stirrer for 1-2 h, and then cooled to 15-20 C. at a rate of 5-10 C./h for crystallization. It was sampled to be analyzed by HPLC every 1-2 h until wt % of the mother liquid was ?3% or the change of the wt % between consecutive samples was ?0.5%. The mixture was then filtered with a centrifuge. The filter cake was washed with n-heptane (45.0 kg). The filtrate was transferred into a glass-lined reactor and concentrated at ?45 C. under reduced pressure (?-0.06 MPa) until no more distillate was observed (approximately 20 L remained). Isopropyl acetate (20.0 kg) was added, the mixture was heated to 45-55 C. and stirred for 0.5-1 h. The mixture was dried at 40-50 C. to give tert-butyl 4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate as grey solid (50.65 kg, 76.3% yield), HPLC rt=18.93 min, 99.9% pure, 100% de, 100% ee. The HPLC conditions are given in Table 1 below.

As the paragraph descriping shows that 1001180-21-7 is playing an increasingly important role.

Reference£º
Patent; Genetech, Inc.; Babu, Srinivasan; Gosselin, Francis; Ran, Yingqing; Remarchuk, Travis; Savage, Scott J.; Stults, Jeffrey; Yajima, Herbert; US2015/99880; (2015); 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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

3-(Trans-4-tert-butoxycarbonylamino-cyclohexyl)-propanoic acid (50 mg, 0.18 mmol) and 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (140 mg, 0.37 mmol) were dissolved in a mixture of dimethylacetamide (1.2 mL) and dichloromethane (0.3 mL). Next, diisopropylethylamine (100 muL, 0.55 mmol) was added. After 5 min, a solution of 1-(4-trifluormethyl-phenyl)-piperazine (50 mg, 0.22 mmol) in dimethylacetamide (1.2 mL) and dichloromethane (0.3 mL) was added, and the resulting mixture was stirred at room temperature for 30 min. The mixture was then diluted with dichloromethane (40 mL), and the organic layer was washed with water (2×20 mL), washed with saturated aqueous ammonium chloride (20 mL), washed with water (10 mL), washed with saturated aqueous hydrogencarbonate (2×20 mL), and washed with water (10 mL). The organic phase was dried over magnesium sulfate, filtered, and concentrated under vacuum. The crude product was purified by column chromatography on silica gel (pentane/ethyl acetate, 5:1), and the desired product was isolated as a light yellow solid (68 mg, 76% yield).

30459-17-7, The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; INTERVET INTERNATIONAL B.V.; WO2009/77527; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

tert-butyl 4-(3-benzyl-7-(methylsulfonyl)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)piperidine-1-carboxylate (7) (1g, 2mmol) was added sec-butyl alcohol containing 10mL sealed vial, was added successively 2-methoxy-4-(4-methylpiperazin-1-yl)aniline ( 531mg, 2.4mmol) and TFA (180muL, 2.4mmol).It was heated to 110C, stirred for 18 hours. Cooled to room temperature, poured into 10% NaHCO3Aqueous solution, extracted with methylene chloride twice, combined organic phase was washed with water twice and saturated brine, dried over anhydrous Na2SO4Dried, filtered and spin dry, column chromatography solid 0.684g (53.3%).

122833-04-9, The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangzhou Institute of biomedicine and health, Chinese Academy of Sciences; Ding, Ke; Xu, Shilin; Xu, Tianfeng; Zhang, Lianwen; Ding, Fang; Tu, Zhengchao; Lu, Xiaoyun; Ding, Jian; Geng, MeiYu; (82 pag.)CN104418860; (2016); B;,
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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Compound 9 (10g, 82.6mmol) placed in 500mL single-port flask, 200mLDMSO. At room temperature was added (2R, 6S) -2,6-dimethylpiperazine (14g, 124mmol) and K2CO3 (28.5g, 206.5mmol), and mix well. Then heated to 130 , reaction 8h. After completion of the reaction was poured into 1L of water. (150mL * 3) and extracted three times with ethyl acetate. The organic phase was washed with 100mL saturated brine, dried over anhydrous sodium sulfate, the solvent spin dried to give a yellowish solid 15g, yield 85%.

21655-48-1, The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ShangHai HaiHe Pharmaceutical Co., Ltd.; Shanghai Institute of Materia Medica Chinese Academy of Sciences; Geng, Meiyu; Liu, Lei; Jiang, Lei; Huang, Min; Chua, Chuantao; Ai, Jing; Wang, Lei; Cao, Jianhua; Ding, Jian; (58 pag.)CN105524048; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,74879-18-8

(S)-2-Methylpiperazine (CAS No 74879-18-8) (420mg) is added to a solution ofIntermediate 7 (1g) in a mixture of NMP (10ml) and TEA (0.5 ml). The mixture is stirred for 1h at room temperature and then added to water (40ml). The mixture is stirred for 30 min, then the product is collected by filtration and washed with water (2 x 20ml) to give the title compound as colourless solid (H Og1 92 %). LCMS 402/404 [M+H]+, RT 2.64 mins (pH 5.8). 1 H NMR 300 MHz (d6-DMSO) (delta ppm): 9.65 (1 H, br s), 7.95 (1 H, m), 7.85 (1 H, d), 7.68 (1 H, dd), 4.75 (2H, m), 3.00-3.15 (2H, m), 2.70-2.82 (3H, m), 2.50 (1H, br s), 1.23 (9H, s), 1.07 (3H1 d)

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; UCB PHARMA, S.A.; WO2008/74445; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution containing 2 7g (18 9 mmol) of 1-[2-(methyloxy)ethyl]piotaperaziotane and 20 mL of THF at O0C was added 0 9 g (23 mmol) of a 60% suspension of sodium hydride in mineral oil The reaction mixture was allowed to stir for 15 mm and 3 O g (18 9 mmol) of 2-chloro-5-niotatropyriotadiotane was added The reaction mixture was heated at 60 0C overnight and then quenched by the addition of H2O and extracted with EtOAc The combined organic layers were dried over MgSO4 and the solvents were removed under reduced pressure The residue was subjected to silica gel chromatography to give 2 7g (54%) of 1-[2-(methyloxy)ethyl]-4-(5-niotatro-2- pyriotadiotanyl)piotaperaziotane as a yellow solid 1 H-NMR (400 MHz, DMSO-cfe) delta 8 95 (d, J = 2 8 Hz, 1 H), 8 21 (dd, J = 9 6 and 2 8 Hz, 1 H), 6 94 (d, J = 9 7 Hz, 2 H), 3 71 – 3 78 (m, 4 H), 3 46 (t, J = 5 7 Hz, 2 H), 3 24 (s, 3 H), and 2 50 – 2 53 (m, 6 H)

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXOSMITHKLINE LLC; ADJABENG, George; BAUM, Erich; BIFULCO, Neil; DAVIS-WARD, Ronda, G.; DICKERSON, Scott, Howard; DONALDSON, Kelly, Horne; HORNBERGER, Keith; PETROV, Kimberly; RHEAULT, Tara, Renae; SAMMOND, Douglas, McCord; SCHAAF, Gregory, M.; STELLWAGEN, John; UEHLING, David, Edward; WATERSON, Alex, Gregory; WO2010/104899; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1. tert-butyl 4-({[(2S,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]oct-2-yl]carbonyl}amino)piperazine-1-carboxylate (206) To a solution of (2S,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid 1 (0.17 g, 0.615 mmol) in dry DCM (10 mL) were added tert-butyl 4-aminopiperazine-1-carboxylate 205 (0.19 g, 0.923 mmol), 1-hydroxybenzotriazole (0.125 g, 0.923 mmol), 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (0.177 g, 0.923 mmol) and 4-dimethylaminopyridine (0.113 g, 0.923 mmol) at room temperature. The reaction mixture was stirred at room temperature overnight, and then concentrated under vacuum. The residue was purified by column chromatography to give tert-butyl 4-({[(2S,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]oct-2-yl]carbonyl}amino)piperazine-1-carboxylate 206 (0.25 g, 88%) as a clear thick oil. 1H NMR (400 MHz, CDCl3): delta 1.46 (9H, s), 1.62 (1H, m), 1.95 (2H, m), 2.38 (1H, m), 2.70 (1H, d, J=12.0 Hz), 2.76 (4H, m), 2.99 (1H, d, J=12.0 Hz), 3.30 (1H, m), 3.57 (4H, m), 3.89 (1H, d, J=8.0 Hz), 4.90 (1H, d, J=11.6 Hz), 5.04 (1H, d, J=12.0 Hz), 7.21 (5H, m), 8.90 (1H, br s).

118753-66-5, The synthetic route of 118753-66-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NAEJA PHARMACEUTICAL INC.; MAITI, Samarendra N.; Nguyen, Dai; Khan, Jehangir; Ling, Rong; US2013/225554; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics