Month: April 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

The tert-butyl 4-{4-[(3-hydroxypropyl)carbamoyl]phenyl}piperazine-1-carboxylate required for the synthesis was prepared as follows: 4-{4-[(tert-butoxy)carbonyl]piperazin-1-yl}benzoic acid (1 g, 3.26 mmol) was dissolved in DMF (15ml) and DIPEA (1.62 ml, 9.79 mmol) and HATU (1489.38 mg, 3.92 mmol) were added to the mixture and stirred at room temperature for 30 minutes. 3-aminopropan-1-ol (0.5 ml, 6.53 mmol) is added and the reaction is stirred for further 2 hours. Mixture is diluted with water (10ml) and extracted with ethyl acetate (10×3 ml), the organic layers are combined and washed with water (2x10ml), dried over magnesium sulphate, filtered and reduced in vacuo. The remaining residue is sonicated with heptane and DCM to remove the remaining traces of DMF, yielding 1.1 g, 93% of the title compound as an orange solid. METCR1673 Generic 2 minutes M/Z (ES+) 364.15, Retention time 1.12. 1H NMR (500 MHz, DMSO-d6) delta 8.16 (t, J = 5.6 Hz, 1H), 7.73 (d, J = 8.9 Hz, 2H), 6.96 (d, J = 9.0 Hz, 2H), 4.46 (t, J = 5.3 Hz, 1H), 3.45 (q, J = 6.2 Hz, 6H), 3.31 – 3.26 (m, 2H), 3.27 – 3.21 (m, 4H), 1.66 (p, J = 6.5 Hz, 2H), 1.43 (s, 9H).

162046-66-4, The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK PATENT GMBH; SUTTON, Amanda; WALTER, Daryl; EAST, Steve; PEREZ, Yolanda; (133 pag.)WO2017/45750; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Compound 4 0.2 g (0.41 mmol) and 25 muL piperdine (0.82 mmol) was added to the 1.0 mL dried CH2Cl2.Anhydrous Na2CO3 20 mg was then added to the mixture, which was stirred for 12 h. The mixturewas washed with the distilled water, the organic phase was separated and dried over anhydrousNa2SO4, and then concentrated viarotary evaporation. The crude product was purified by silica gelchromatography with petroleum ether?acetone?strong ammonia water (v/v/v, 8/1/0.1) as the eluentto gain 0.18 g yellow solid compound 5a in 90percent yield.

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

Reference£º
Article; Feng, Xiu E.; Wang, Qin Jin; Gao, Jie; Ban, Shu Rong; Li, Qing Shan; Molecules; vol. 22; 12; (2017);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,76003-29-7

step 1: To a mixture of NaH (430 mg, 1.8 mmol) in DMF (5 mL) was added tert-butyl 3-oxopiperazine-1-carboxylate (3.0 g, 1.5 mmol) and 2-bromoacetonitrile (1.8 g, 1.5 mmol) at 0 C. The mixture was stirred at RT overnight. The reaction mixture was then diluted with EtOAc (10 mL) and H2O (10 mL). The separated organic layer was washed with brine, dried (MgSO4), filtered and concentrated in vacuo. The residue was purified by SiO2 chromatography eluting with DCM/MeOH (40:1) to afford tert-butyl 4-(cyanomethyl)-3-oxopiperazine-1-carboxylate as yellow oil (3.0 g, 76%). LCMS (ESI): m/z=240.1 [M+1]+

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GENENTECH, INC.; Rudolph, Joachim; Gazzard, Lewis J.; Crawford, James J.; Ndubaku, Chudi; Drobnick, Joy; Lee, Wendy; US2015/31674; (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.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

(S)-3-(hydroxymethyl)-6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-one (150 mg, 0.684 mmol), 1-(2,4-difluorophenyl)piperazine (136 mg, 0.684 mmol), (cyanomethyl)trimethylphosphonium iodide (249 mg, 1.026 mmol) and N,N-diisopropylethylamine (0.597 ml, 3.42 mmol) were suspended in propionitrile (2 ml) and heated in a closed vial at 90 C. for 2 h. The reaction mixture became a clear dark brown solution. It was cooled to room temperature, diluted with DMSO (2 mL) and purified using preparative HPLC (25-95% acetonitrile in water, NH4HCO3 buffered). The fractions containing product were concentrated in vacuo and crystallized from water (3 mL). The precipitate was filtered and dried in vacuum to afford (S)-3-((4-(2,4-difluorophenyl)piperazin-1-yl)methyl)-6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-one (63.2 mg, 0.158 mmol, 23.13% yield) as a light brown solid. 1H NMR (400 MHz, DMSO-d6) delta (ppm): 1.84-2.03 (m, 3H) 2.09-2.26 (m, 1H) 2.41-2.49 (m, 4H) 2.88-2.99 (m, 4H) 3.34-3.43 (m, 3H) 3.54-3.63 (m, 1H) 3.94-4.02 (m, 1H) 6.93-7.09 (m, 3H) 7.18 (ddd, J=12.44, 9.16, 2.91 Hz, 1H) 7.61 (d, J=1.77 Hz, 1H) 10.44 (s, 1H); [M+H] calc’d for C21H23F2N5O, 400; found, 400.

115761-79-0, The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; US2010/190763; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (2i?,65)-2,6-dimethylpiperazine (8.0 g, 70.1 mmol) in DCM (70 niL) was added triethylamine (9.78 niL, 70.1 mmol). The reaction mixture was cooled to 0 0C and benzyl chlorocarbonate (9.86 mL, 70.1 mmol) was added. After stirring at 0 0C for 1 hour, the reaction was warmed to rt. The reaction mixture was washed with brine, dried (Na2SO4), concentrated and the residue purified with silica chromatography (Hex:EtOAc 1 :1 to EtOAc to EtOAc:MeOH 10:1) to give 13.48g (77 percent) of a colorless oil

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; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/136191; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5625-67-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

To a stirred solution of W-l (20.0 g, 0.200 mol) in DCM, is added Boc anhydride (43.6 g, 0.200 mol), and TEA (40.4 g, 0.400 mol). The mixture is stirred at about 25 C for about 18 hours. The mixture is concentrated and the residue dissolved in EtOAc then extracted with water. The organic layer is concentrated and the residue is purified by silica gel chromatography to give W-2.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BRUNETTE, Steven, Richard; ABEYWARDANE, Asitha; BURKE, Michael, J.; KAPADIA, Suresh, R.; KIRRANE, Thomas, Martin, Jr.; NETHERTON, Matthew, Russell; RAZAVI, Hossein; RODRIGUEZ, Sonia; SAHA, Anjan; SIBLEY, Robert; SMITH KEENAN, Lana, Louise; TAKAHASHI, Hidenori; TURNER, Michael, Robert; WU, Jiang-Ping; YOUNG, Erick, Richard, Roush; ZHANG, Qiang; ZHANG, Qing; ZINDELL, Renee, M.; WO2013/134226; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

159532-59-9, (S)-1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 43: r(2S)-1-methyl-2-piperazinynmethanol; (2S)-1-{[(1 , 1-dimethylethyl)oxy]carbonyl}-2-piperazinecarboxylic acid (Commercial from ACESYS) (1.03 g, 4.47 mmol) was dissolved in dry Tetrahydrofuran (THF) (25 ml) and cooled to 0C under nitrogen. Lithium aluminium hydride (1 1 ml, 11.00 mmol) was added dropwise and the reaction was stirred at 0C for 15mins and allowed to warm to room temperature. The solution was stirred for ~1 hour at room temperature and then heated at reflux overnight. TLC (20% MeOH/DCM + few drops ammonia; visualised by KMn04) showed the reaction had gone to completion.After cooling, the reaction was cooled to 0C and quenched by the dropwise sequential addition of water (0.5ml), 2M NaOH (0.5ml) and water (1 ml). The resulting slurry was filtered and washed with THF. The filtrate was evaporated in vacuo and the resulting oil was azeotroped with methanol (x2) to give the title compound as colourless oil (374mg)LCMS (Method B): Rt = 0.18 min, MH+ = 131, 159532-59-9

The synthetic route of 159532-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; ATKINSON, Francis Louis; ATKINSON, Stephen John; BARKER, Michael David; DOUAULT, Clement; GARTON, Neil Stuart; LIDDLE, John; PATEL, Vipulkumar Kantibhai; PRESTON, Alexander G; SHIPLEY, Tracy Jane; WILSON, David Matthew; WATSON, Robert J; WO2012/123312; (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.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: To a well-stirred solution of intermediate 5a (2.0 g,5.29 mmol) in ethanol (10 mL) was added 1-amino-4-methylpiperazine 9a (0.61 g, 5.29 mmol) and a drop of acetic acid,and the mixturewas stirred at 78 C for 2 h. The mixturewas cooledto room temperature and the resulting solid was collected byfiltration and purified by column chromatography to give the targetcompounds 6a-1 as a yellow solid in 75% yield. M.p: 228-230 C;, 118753-66-5

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

Reference£º
Article; Wu, Yachuang; Ding, Xiudong; Yang, Yifeng; Li, Yingxiu; Qi, Yinliang; Hu, Feng; Qin, Mingze; Liu, Yajing; Sun, Lu; Zhao, Yanfang; European Journal of Medicinal Chemistry; vol. 185; (2020);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The starting material was prepared as follows: 3-Bromopropan-1-ol (20 ml, 20 mmol) was added dropwise to a solution of 1-methylpiperazine (29 ml, 26 mmol) in ethanol (200 ml). Potasium carbonate (83 gr, 60 mmol) was added and the mixture was refluxed for 20 hours. After cooling, the solid was filtered and the filtrate was evaporated. The residue was triturated with ether, filtrate and evaporated. The residue was distilled at about 60-70 C. under about 0.2 mm Hg to give 1-(3-hydroxypropyl)-4-methylpiperazine (17 g, 53%). 1H NMR Spectrum: (CDCl3) 1.72 (m, 2H); 2.3 (s, 3H); 2.2-2.8 (in, 8H); 2.6 (t, 2H); 3.8 (t, 2H); 5.3 (br s, 11H)

109-01-3, The synthetic route of 109-01-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hennequin, Laurent Francois Andre; US2003/212055; (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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Intermediate 45: 1,1-dimethylethyl (3S)-4-ethyl-3-(hydroxymethyl)-1-piperazinecarboxylate 1,1-dimethylethyl (3S)-3-(hydroxymethyl)-1-piperazinecarboxylate (Commercial: e.g. Activate Scientific) (0.5 g, 2.312 mmol) and acetaldehyde (0.209 ml, 3.70 mmol) were dissolved in Methanol (10 ml) with molecular sieves and stirred at room temperature under nitrogen for 4 hours. Sodium borohydride (0.140 g, 3.70 mmol) was added and the reaction was stirred at room temperature for 18 hours. The reaction was quenched with 2M NaOH and the reaction was filtered through a celite column. The filtrate was extracted with ethyl acetate (*3). The combined organics were washed with water, dried using a hydrophobic frit and evaporated in vacuo to give the title compound as a colourless oil (0.546 g) LCMS (Method B): Rt=0.45 min, MH+=245

314741-40-7, As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference£º
Patent; GLAXO GROUP LIMITED; Atkinson, Francis Louis; Atkinson, Stephen John; Barker, Michael David; Douault, Clement; Garton, Neil Stuart; Liddle, John; Patel, Vipulkumar Kantibhai; Preston, Alexander G.; Shipley, Tracy Jane; Wilson, David Matthew; Watson, Robert J.; US2014/5188; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics