Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.60787-05-5,1-(4-Methylpiperazin-1-yl)ethanone,as a common compound, the synthetic route is as follows.,60787-05-5

To a solution of 1 -(4-methylpiperazin-1 -yl)ethanone (1 .68 g, 1 1 .8 mmol) in THF (25 mL) cooled to -78 C, a solution of LDA (1 .5 M in THF, 9.8 mL, 14.75 mmol) was added, and the resulting mixture was stirred at -78 ^ for 1 h under argon atmosphere. Finally, a solution of 4-bromoindan-1 -one (1 .25 g, 5.9 mmol) in THF (50 mL) was added, and the resulting mixture was kept at -78 ‘ for 4 h. The reaction mixture was diluted with water and extracted with EtOAc. The organic extracts were dried over Na2S04 and evaporated to dryness. A solution of the previous residue in AcOH:H2S04:H20 (79 mL, 85:10:5) was stirred for 6 h. The reaction mixture was poured into water, basified with 50% NaOH and extracted with EtOAc. The organic extract, after being dried over Na2S04, was evaporated to dryness. To a solution of the previous residue in THF (75 mL) cooled to 0 C, AIH3- NMe2Et (0.5 M in toluene, 20 mL, 10.34 mmol) was added and the resulting mixture was stirred for 5 h. EtOAc:H20 (90 mL, 1 :1 ) was added to the reaction mixture and the resulting suspension was filtered through Celite. The layers were separated and the aqueous phase was extracted with EtOAc. The organic extract was dried over Na2S04 and evaporated to dryness. A solution of the previous residue in 37% HCLEtOH (150 mL, 1 :1 ) was refluxed overnight. The reaction mixture was evaporated to dryness. Purification of the residue by silica gel column chromatography (EtOAc/NH3:MeOH mixtures of increasing polarity as eluent) afforded the desired product (981 mg, 51 %). 1 H-NMR (CDCI3, 300 MHz) delta: 7.32 (m, 2H), 7.18 (t, J= 7.6 Hz, 1 H), 6.30 (s, 1 H), 3.31 (d, J= 1 .8 Hz, 2H), 2.72 (m, 4H), 2.60 (m, 4H), 2.51 (m, 4H), 2.30 (s, 3H) ppm. EI-MS m/z: 320.1 (M).

As the paragraph descriping shows that 60787-05-5 is playing an increasingly important role.

Reference£º
Patent; LABORATORIOS DEL DR. ESTEVE, S.A.; ALCALDE-PAIS, Maria, de las Ermitas; ALMANSA-ROSALES, Carmen; DIAZ-FERNANDEZ, Jose-Luis; MESQUIDA-ESTEVEZ, Maria, de les Neus; PALOMA-ROMEU, Laura; WO2014/6071; (2014); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.,5464-12-0

Example 43 2-(4-Methylpiperazin-1-yl)ethyl 4-(4-chlorobenzyl)piperazine-1-carboxylate 2-(4-Methyl-piperazin-1-yl)-ethanol (0.86 g, 6 mmol) and NMM (0.58 mL, 6 mmol) were dissolved in DCM (8 mL) and the reaction mixture was cooled to 0¡ã C. 4-Nitrophenyl chloroformate (1.29 g, 6 mmol) was added and stirred for 1 h. To the reaction mixture was added a solution of 1-(4-chloro-benzyl)-piperazine (1.05 g, 5 mmol) and DIPEA (6.0 mL, excess) in DMF (20 mL). The reaction mixture was stirred at room temperature overnight and then concentrated in vacuo. The residue was dissolved in EtOAc (150 mL), washed with sat aq Na2CO3 solution (6*100 mL), dried (MgSO4) and dried in vacuo. The residue was initially purified by column chromatography (normal phase, 20 g, Strata SI-1, silica gigatube, 20 mL/min, gradient 0percent to 15percent MeOH in DCM) and then further purified by reverse phase column chromatography (LiChroprep RP-18, 40-63 mum, 460*26 mm (100 g), 30 mL/min, gradient 0percent to 30percent (over 40 min) MeOH in water with 1percent formic acid). The residue was stirred for 2 h in DCM (10 mL) with K2CO3 (~0.20 g), filtered and then dried in a vacuum oven overnight to give 2-(4-methylpiperazin-1-yl)ethyl 4-(4-chlorobenzyl)piperazine-1-carboxylate (0.51 g, 28percent) as a pale yellow oil. Analytical HPLC: purity 99.7percent (System A, RT=3.39 min); Analytical LCMS: purity 100percent (System A, RT=3.83 min), ES+: 381.5 [MH]; HRMS calcd for C19H29ClN4O2: 380.1979, found 380.1996.

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Biovitrum AB; US2009/281087; (2009); A1;,
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3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a) 1,4-Bis(tert-butoxycarbonyl)-2-piperazinecarboxylic acid To a solution of piperazine-2-carboxylic acid dihydrochloride (5 g, 24.6 mmol) in 2M sodium hydroxide (40 mL) and ethanol (40 mL) was added di-tert-butyl dicarbonate (11.82 g, 54.1 mmol) and the reaction mixture stirred for 3 days. The organic solvent was removed in vacuo, the aqueous phase basified with 2M sodium hydroxide and extracted with diethyl ether to remove excess di-tert-butyl dicarbonate. The aqueous layer was adjusted to pH 3-4 and extracted with ethyl acetate. The combined organic extracts were dried (MgSO4), filtered and evaporated to yield 1,4-bis(tert-butoxycarbonyl)-2-piperazinecarboxylic acid as a white solid.

3022-15-9, As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference£º
Patent; Agejas-Chicharro, Javier; Belen Bueno Melendo, Ana; Camp, Nicholas Paul; Gilmore, Jeremy; Jimenez-Aguado, Alma Maria; Lamas-Peteira, Carlos; Marcos-Llorente, Alicia; Mazanetz, Michael Philip; Montero Salgado, Carlos; Timms, Graham Henry; Williams, Andrew Caerwyn; US2004/122001; (2004); 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.

Step B tert-Butyl (3S)-3-methylpiperazine-1-carboxylate To a solution of (2S)-2-methylpiperazine (20.0 g, 0.200 mol) in methylene chloride (300 mL) and triethylamine (20.4 g, 0.202 mol) was added dropwise a solution of di-tert-butyl dicarbonate (44.0 g, 0.202 mol) in CH2Cl2 (100 mL) over 5 hrs. The mixture was washed with water, brine, and then dried over MgSO4 and concentrated. Column chromatography on silica (10-20% MeOH in EtOAc) afforded 32.0 g (80%) of the title compound as an oil. Step C tert-Butyl (3S)-4-(5-bromo-2,3-dihydro-1H-inden-1-yl)-3-methylpiperazine-1-carboxylate, 74879-18-8

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

Reference£º
Patent; Xue, Chu-Biao; Cao, Ganfeng; Huang, Taisheng; Chen, Lihua; Zhang, Ke; Wang, Anlai; Meloni, David; Anand, Rajan; Glenn, Joseph; Metcalf, Brian W.; US2005/261310; (2005); A1;,
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5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-Chloro-5-nitropyridine (800 mg, 5.05 mmol) was dissolved in dioxane (20 mL) and then 1-ethylpiperazine (1.7 g, 15.15 mmol) and N,N-diisopropylethylamine (927 mL, 5.05 mmol) were added. The reaction mixture solution was stirred at 70 C for a day. The reaction solution was cooled to room temperature, diluted with ethyl acetate, and then washed with brine. The organic layer was concentrated by drying with magnesium sulfate. The target compound (1.05 g, 87% yield) was used in the following reaction without purification. [0166] MS m/z: 237.51 [M+1].

5308-25-8, The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY; SIM, Tae Bo; CHOI, Hwan Geun; HAH, Jung Mi; HAM, Young Jin; JUN, Eun Jin; LEE, Jung Hun; KIM, Hwan; WO2011/49332; (2011); 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.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 1a-c (1.93 g, 10 mmol), 4 (1.76 g, 10mmol) and KF (18 mmol) were heated at 120-130 ¡ãC inDMF (30 mL) for 16 – 18 h. At the end of this period, thereaction mixture was cooled to room temperature and dilutedwith water (30 mL). The separated solid was filtered, washedand dried to obtain crude 5a-i. The obtained crude productwas then purified by recrystallization using ethanol

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

Reference£º
Article; Darsi, S.S. Praveen Kumar; Kumar, K. Shiva; Devi, B. Rama; Naidu; Dubey; Letters in Organic Chemistry; vol. 11; 8; (2014); p. 551 – 555;,
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.304897-49-2,tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

2,4-Dichloro-5-(trifluoromethyl)pyrimidine (0.546 g, 2.52 mmol) in 1 : 1 dichioroethane: fe/f-butanol was cooled to 0 C under nitrogen. A 1.0 M solution of zinc(ll) chloride in diethyl ether (3.43 mL, 3.34 mmol) was added, and the mixture stirred for one hour at 0 C. iert-Butyl 4-(4-aminobenzyi)piperazine-1-carboxylate (193) (0.667 g, 2.29 mmol) in 1 : 1 dichioroethane: ferf-butanol (20 mL) vv’as added dropwise over thirty minutes, followed by triethyiamine (0.351 mL, 2.52 mmol) in 1 :1 dichioroethane: ferf-butanol (10 mL). The mixture was stirred overnight, allowing the ice bath to come to room temperature over this time. The mixture was concentrated onto silica gel and chromatographed (40 g silica cartridge, 0-100% ethyl acetate/petroleum benzine 40- 60 C) to give a residue which was triturated with petroleum benzine 40-60 C to give the title compound {194) (0.976 g, 90%) as an off white solid; 1H NMR (400 MHz, dr MeOD) delta 8.68 (d, J = 0.6 Hz, 1 H), 7.85 (d, J = 8.6 Hz, 2H), 7.51 (d, J = 8.6 Hz, 2H), 4.30 (s, 2H), 3.27 – 3,00 (br, overlaps with solvent), 1.47 (s, 9H). LCMS Method C: 5.08 min; m/z 472.1 [M+H]+; m/z 470.1 [M-H]

304897-49-2, 304897-49-2 tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate 12045001, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CANCER THERAPEUTICS CRC PTY LTD; DEVLIN, Mark Graeme; STREET, Ian Philip; TONG, Warwick Bonner; WO2014/27199; (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.1188265-73-7,tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Phenyl (4-chloro-3-fluorophenyl)carbamate (441 mg, 1.659 mmol) and tert-butyl 3-(2- hydroxyethyl)piperazine-l-carboxylate (382 mg, 1.659 mmol) were suspended in EtOH (5 niL) and heated in a Biotage Initiator using initial high setting to 100 C for 7 min. The reaction was concentrated under a stream of nitrogen at 50 C then dissolved in DCM (3 niL) and TFA (3 niL, 38.9 mmol). After 30 minutes the reaction was concentrated under a stream of nitrogen at 50 C. The residue was dissolved in DCM/MeOH and loaded onto a SCX-3 cartridge (2 g). The cartridge was washed with 3 volumes of MeOH, then eluted with 3 volumes of 2N NH3MeOH. The eluants were concentrated under a stream of nitrogen at 50 C followed by high vacuum, resulting in the isolation of N-(4-chloro-3-fluorophenyl)-2-(2 -hydro xyethyl)piperazine-l-carboxamide (494 mg, 1.637 mmol, 99 % yield) as a white solid.LC/MS (ESI): m/z 302.0 (M+H)+, 0.39 min (ret. time)

1188265-73-7, 1188265-73-7 tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate 53407692, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; BAILEY, James; CHEN, Yao; HURLE, Mark; LEACH, Craig; TURUNEN, Brandon; (103 pag.)WO2018/134731; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 IX 20.3 g (0.064 mol), 15.8 g (0.13 mol) DMAP, 20.9 g were added to a 2 L reaction flask.(0.11 mol) EDCI and 500 mL dichloromethane (DCM),The system was stirred at 20 C.A solution of 37.5 g (0.064 mol) of compound VIII and 23.7 g (0.23 mol) of triethylamine and 200 mL of dichloromethane prepared in advance was slowly added dropwise to the above system.After the completion of the dropwise addition, the mixture was stirred at 20 C for 3 hours, and then controlled by HPLC or TLC. The starting material was completely reacted.To the system was added 14.1 g of N,N’-dimethylethylenediamine.The system is heated to 35 C and stirring is continued.After the temperature is stable, add 200 mL of 12% acetic acid solution.After stirring for 10 min, the layers were separated, and the organic layer was washed with 5% sodium hydrogen carbonate solution (200 mL) and then washed with 5% sodium chloride solution (200 mL).The organic layer was dried, filtered, and evaporated to dryness.After the system is heated to 30 C, the methanol solution is added dropwise.After the system is clarified, start to cool down to 0-5 C, and stir for 1 h.After filtration, the cake was dried to give a white solid compound I about 50.8 g.The yield is 91.4%,, 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; Jiangsu Zhongbang Pharmaceutical Co., Ltd.; Huang Shuang; Yang Jian; Wu Xiaogang; Shi Lingyun; Liu Liping; (21 pag.)CN108997333; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

438631-77-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.438631-77-7,(R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

(R)-l-(4-Chlorophenyl)-piperazine-2-carboxylic acid methyl esterR-4N-Boc-piperazine 2-carboxylic acid methyl ester (4.0gms, 16.4mmol) and 4- chlorophenylboronic acid (5.0gms, 32.8mmol) are mixed in dichloromethane (5OmI) . followed by addition of cupric acetate (3.0gms, 16.4mmol), 4 A molecular sieves (1 gm) and pyridine (3.28ml, 32.8mmol). The mixture is stirred at room temperature for 50 hr. The reaction mixture is concentrated directly in vacuo, diluted with ethyl acetate, and filtered through Celite. The organic filtrate is concentrated and the remaining residue is purified over silica gel column chromatography eluting with hexane and ethyl acetate to give 860 mg as a white solid.

As the paragraph descriping shows that 438631-77-7 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GmbH; WO2007/120595; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics