Month: April 2021

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

(0122) To a mixture of Compound 3J (59.8 mg, 0.105 mmol), Compound 11B (33 mg, 0.105 mmol) and N,N-dimethylpyridin-4-amine (38.4 mg, 0.314 mmol) in dichloromethane (5 ml) was added 1-ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (24.07 mg, 0.13 mmol). The reaction mixture was stirred at room temperature overnight and concentrated. The residue was purified by reverse phase HPLC on a C18 column using a gradient of 40-60% acetonitrile/0.1% trifluoroacetic acid in water to give the title compound as the trifluoroacetate salt. The trifluoroacetic acid salt was dissolved in dichloromethane (6 ml) and washed with 50% aqueous NaHCO3. The organic layer was dried over anhydrous Na2SO4 and concentrated to give the title compound. 1H NMR (500 MHz, dimethylsulfoxide-d6) delta 11.68 (s, 1 H), 11.40 (s, br, 1 H), 8.53-8.58 (m, 2 H), 8.04 (d, 1 H), 7.80 (dd, 1 H), 7.47-7.54 (m, 3 H), 7.34 (d, 2 H), 7.02-7.09 (m, 3 H), 6.67 (dd, 1 H), 6.39 (dd, 1 H), 6.19 (d, 1 H), 3.79 (dd, 1 H), 3.69-3.73 (m, 1 H), 3.22-3.37 (m, 3 H), 3.16-3.21 (m, 1 H), 3.07 (s, 4 H), 2.74 (s, 2 H), 2.09-2.24 (m, 6 H), 1.95 (s, 2 H), 1.86-1.93 (m, 1 H), 1.79-1.85 (m, 1 H), 1.58-1.64 (m, 1 H), 1.42-1.51 (m, 1 H), 1.38 (t, 2 H), 1.25-1.34 (m, 1 H), 0.92 (s, 6 H).

1235865-77-6, As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference£º
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
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.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

A solution of 5-fluoro-2-nitroanisole (200 g, 1 eq) and piperazine (302 g, 3 eq) in DMF was stirred for 30 minutes and heated for 12 hours. Acetic anhydride (358 g, 3 eq) was slowly added to the reaction solution, and the reaction solution was stirred at room temperature for 12 hours. Water was added to the reaction solution for dilution, and the solid was filtered and washed twice with water. After drying at 50 C, the product was obtained as a yellow solid (284 g, 87%)., 13889-98-0

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference£º
Patent; Anqing Yuanqi Pharmaceutical Technology Co., Ltd.; Jin Wei; Liu Jinlun; Wang Jianbing; (6 pag.)CN110294721; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 15 1 -mesyl-4-(5-methoxycarbonyl-2-pyridyl)piperazine 1-Mesylpiperazine hydrochloride (4.24 g) was added to a solution of methyl 6-chloronicotinate (1.7 g) and N,N-diisopropylethylamine (6.3 ml) in dimethylacetamide (20 ml) and the mixture was heated at 120 C. for 2 hours.. The mixture was allowed to cool to ambient temperature and poured onto crushed ice/water (50 ml) to precipitate a tan solid.. The solid was collected by filtration and dried at 80 C. for 18 hours in a vacuum oven, to give 1-mesyl-4-(5-methoxycarbonyl-2-pyridyl)piperazine (2.05 g), mp 205-207 C. NMR (d6-DMSO): 2.90 (s, 3H), 3.20 (m, 4H), 3.78 (m, 3H), 3.80 (s, 3H), 6.92 (d, 1H), 8.00 (dd, 1H), 8.67 (d, 1H), m/z 300 (M+1)., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AstraZeneca AB; US6734184; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8,694499-26-8, 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

Step 90.1 : 7-(6-Chloro-pyrimidi?-4-yloxy)-isoquinoli?e-4-carboxylic acid [4-(4-methyl- piperazi?-1-ylmethyl)-3-trifluoromethyl-phenvn-amide; A mixture of 1.95 g (5.5 mMol) 7-(6-chloro-pyrimidin-4-yloxy)-isoquinoline-4-carboxylic acid (Step 93.2), 1.5 g (5.49 mMol) 4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl- phenylamine and 6.42 ml (46.2 mMol) triethylamine in 50 ml dry DMF is heated under an argon atmosphere at 50 C. A solution of 5.4 ml (8.2 mMol) propylphosphonic anhydride is then added. After 2 h, the reaction mixture is poured onto an aqueous solution of NaHCO3 and stirred at 0 0C for 1 h. The suspension is then filtered (hyflo) and the solid residue is dissolved in CH2CI2/MeOH 5:1. The solvent is evaporated off under reduced pressure to afford a crude product which is purified by reversed phase MPLC (Bchi system), yielding, after neutralisation with saturated aqueous NaHCO3, the title compound as a orange solid.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2006/59234; (2006); 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.21091-98-5,(4-Methylpiperazin-1-yl)(4-nitrophenyl)methanone,as a common compound, the synthetic route is as follows.

To 1.67 g (6.70 mmol) of the product prepared in step 2.1 partially dissolved in 50 mL of methanol are added, under an inert atmosphere, 71 mg of 10% palladium-on-charcoal. The reaction mixture is stirred at room temperature under 3 bar of hydrogen for 2 hours 30 minutes and then filtered through Celite. After evaporating to dryness, 1.5 g of the expected product are obtained in the form of an orange oil, which is used as obtained in the following step. Quantitative yield., 21091-98-5

21091-98-5 (4-Methylpiperazin-1-yl)(4-nitrophenyl)methanone 716396, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SANOFI; US2012/277220; (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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,74879-18-8

In a sealed tube, 7-fluoro-9-methyl-2-(2-methylimidazo[l,2-b]pyridazin-6-yl)pyrido[l,2- a]pyrimidin-4-one (Intermediate 3; 250 mg, 0.808 mmol), and (S)-2-methylpiperazine (405 mg, 4.04 mmol, 5.0 eq.) were stirred in DMSO (6 mL) and heated at 130C overnight. The solvent was removed under high vacuum. The residue was taken up in CH2C12and washed with an aqueous saturated solution of NaHC03. The organic layer was separated and dried over Na2S04and concentrated in vacuo. The crude was purified by column chromatography (Si02,CH2Cl2/MeOH=95/5 to 85/15) to afford the title product (135 mg, 43%) as a light yellow solid. MS m/z 390.3 [M+H+].

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

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; MCCARTHY, Kathleen Dorothy; METZGER, Friedrich; RATNI, Hasane; (76 pag.)WO2017/81111; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3 -Bromo-5 -nitro-toluene, (7.7 8g, 36.0 mmol) and 1 -cyclopropylpiperazine (5 .0g, 39.6 mmol) were dissolved in 100 mL of dry t-BuOH and purged with N2 for 10 minutes. During the purge added t-BuXphos Palladacycle (620mg, 0.9Ommol) followed by sodium t-butoxide, (5.20g, 54.0 mmol) and reaction was allowed to stir at 30C under N2 for two hours. Solvent was removed under reduced pressure and the residue partitioned between EtOAc and water, then the organic phase washed with brine, dried (Na2504) and solvent removed under reduced pressure. The crude material was Isco purified on 5i02 with DCM changing to isocratic 10%/EtOAc/DCM as eluent to afford 6.75 g (64%) of JW-8a as a dark yellow, waxy solid. ?H NMR (400 MHz, Acetone-d6) oe 7.51 (t, J = 2.1 Hz, 1H), 7.43 (d, J = 0.6 Hz, 1H), 7.21 (s, 1H), 3.35 – 3.18 (m, 4H), 2.83 – 2.67 (m, 4H), 2.40 (s, 3H), 1.75 – 1.59 (m, 1H), 0.57 – 0.41 (m, 2H),0.38 (dt, J = 3.8, 2.5 Hz, 2H) ppm. ESI-MS m/z calc. 261.14774, found 262.0 (M+1)+; Retention time: 0.58 minutes., 20327-23-5

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

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; DAVIES, Robert, J.; CAO, Jingrong; COCKERILL, Meghan, Elise; COLLIER, Philip, Noel; DENINNO, Michael, Paul; DOYLE, Elisabeth; FRANTZ, James, Daniel; GAO, Huai; GOLDMAN, Brian, Anthony; GREY, Ronald, Lee; GRILLOT, Anne-laure; GU, Wenxin; HENDERSON, James, A.; IRARRAZAVAL, Raul Eduardo, Krauss; KOLPAK, Adrianne, Lynn; LIAO, Yusheng; MAGAVI, Sanjay Shivayogi; MALTAIS, Francois; MESSERSMITH, David; PIERCE, Albert, Charles; PEROLA, Emanuele; RYU, Elizabeth Jin-Sun; SYKEN, Joshua; WANG, Jian; (706 pag.)WO2016/197009; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

120737-78-2, Under an argon atmosphere,tert-butyl 2-methylpiperazine-1-carboxylate(1.28 g, 6.40 mmol), 1-bromo-3-fluoro-4-iodobenzene (2.31 g, 7.68 mmol), copper iodide (122 mg, 0.640 mmol)Triopotassium phosphate (4.08 g, 25.6 mmol),Ethylene glycol (716 muL, 12.8 mmol) inA solution of 1-butanol (6 mL) was stirred at 100 C. for 16 h.Water was added to the reaction solution, and the mixture was extracted with ethyl acetate.The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, filtered, and the solvent was distilled off. The resulting residue was purified by silica gel column chromatography (hexane / ethyl acetate) to give the title compound (767 mg, 32%).Clear oil

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Yakult Honsha Corporation; Abe, Atsuhiro; Mae, Satoyuki; Yamazaki, Ryuta; Sawaguchi, Yuichi; Sugimoto, Takuya; Sasai, Toshio; Nishiyama, Hiroyuki; Nagaoka, Masato; Matsuzaki, Ken; Kurita, Akinobu; Matsui, Makoto; Shingeyama, Takahide; (208 pag.)JP6378918; (2018); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 190a tert-Butyl 3,3-Dimethyl-4-(6-nitropyridin-3-yl)piperazine-1-carboxylate 190a A 100-mL single-neck round-bottomed flask equipped with a magnetic stirrer and a reflux condenser was charged with 5-bromo-2-nitropyridine (5.6 g, 28.0 mmol), tert-butyl 3,3-dimethyl-4-piperazine-1-carboxylate (3.0 g, 14.0 mmol), cesium carbonate (9.1 g, 28 mmol), and 1,4-dioxane (50 mL). After bubbling nitrogen through the resulting solution for 30 min, Binap (870 mg, 1.4 mmol) and tris(dibenzylideneacetone)-dipalladium(0) (1.2 g, 1.4 mmol) were added. The reaction mixture was subjected to three cycles of vacuum/argon flush and stirred at 120 C for 24 h. After this time the reaction was cooled to room temperature, filtered and the filtrate was partitioned between ethyl acetate (200 mL) and water (50 mL). The aqueous layer was separated and extracted with ethyl acetate (3 * 50 mL). The combined organic layers were washed with brine (50 mL) and dried over sodium sulfate. The drying agent was removed by filtration and the filtrate was concentrated under reduced pressure. The residue was purified by silica-gel column chromatography eluting with 5:1 petroleum ether/ethyl acetate to afford 190a (1.27 g, 27%). LCMS: [M+H]+ 337.2.

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference£º
Patent; F.Hoffmann-La Roche AG; CRAWFORD, James John; ORTWINE, Daniel Fred; WEI, BinQing; YOUNG, Wendy B.; EP2773638; (2015); B1;,
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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, Di-tert-butyl dicarbonate (3.92 g, 17.98 mmol) was added to a suspension of 2-piperazinone (1.50 g, 14.98 mmol) in dichloromethane (15 mL). The mixture was stirred at room temperature for 5 hours. The solvent was evaporated to afford 1 ,1- dimethylethyl 3-oxo-1-piperazinecarboxylate (2.99 g, quantitative) as an off-white solid.

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

Reference£º
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; PEAT, Andrew, James; PRICE, Daniel, J.; SHOTWELL, John, Brad; TAI, Vincent; ZHANG, Huichang; WO2011/41713; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics