Heterocyclic Building Blocks-piperazine

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;,
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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
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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.,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;,
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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;,
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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;,
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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;,
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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;,
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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 the 1200 L reactor was added [60C] racemic 2-methylpiperazine (100 kg) from a drum. H20 (240 L) was added, and the solution was cooled to [13C.] To the 1200 L receiver was added L-tartaric acid (150 kg). [H20] (140 L) was added, and the slurry was stirred for 1 h 35 min until dissolution of the solids was complete. The L-tartaric acid solution was transferred to the 1200 L reactor over 2 h while maintaining a temperature of [10-22C] in the 1200 L reactor followed by a [H20] rinse (20 L). Ethanol (163 kg) was added to the 1200 L reactor, and the solution was cooled to [2C.] The resulting slurry was stirred for 2 h at [2C,] and filtered through a 36″Nutsche filter sending the filtrate into the 1200 L receiver. The 1200 L reactor and 36″Nutsche filter were washed with H20 (200 L), and the solids were dried to yield 214 kg of 12% ee [(171%] based on the title compound). These solids were recharged to a clean 1200 L receiver and H20 (630 L) was added to the 1200 L receiver, which was heated to [85C] until all the solids had dissolved. The solution was filtered through an in-line filter (C) into the 1200 L reactor, cooled to [5C,] and stirred for 2 h. The resulting slurry was filtered through a clean 36″Nutsche filter sending the filtrate into the 1200 L receiver. The 1200 L reactor and 36″Nutsche filter were washed with [H20] (200 L), and the solids were dried to yield 104 kg of 93% ee (83% based on the title compound). These solids were recharged to a clean 1200 L receiver and [H20] (254 L) was added to the 1200 L receiver, which was heated to [85C] until all the solids had dissolved. The solution was filtered through an in-line filter (C) into the 1200 L reactor, cooled to [5C,] and stirred for 2 h. The resulting slurry was filtered through a clean 36″Nutsche filter sending the filtrate into the 1200 L receiver. The 1200 L reactor and 36″Nutsche filter were washed with H20 (200 L), and the solids were dried to yield 92 kg of 99% ee (74% based on the title compound). [D1] does not describe the preparation of the title compound but makes reference [TO J.] Med. Chem. 1990, 33, 1645-1656 (D2). The yield of the title compound according to D2, starting from racemic 2-methylpiperazine was 35%. M. Pt. 255.0-257. [0C.] ‘H NMR (400 MHz, [D20)] : [6] 4.79 [(D20,] reference), 4.36 (2H, s), 3.73-3. 64 (4H, [M),] 3.43 [(1H,] td J = 13.7, 3.0 Hz), 3.34 [(1H,] td, J = 12.7, 3.1 Hz), 3.17 [(1H,] dd, J = 14.2 12.8 Hz), 1.41 (3H, d, J = 6.1 Hz), 0.00 (TMS, reference). [13C] NMR (100 MHz, [D20)] : [6] 178.46 (s), 73.91 (d), 49.02 (d), 49.00 [(MEOH,] reference), 45.82 (t), 40.56 (t), 40.10 (t), 15.42 (q). IR (diffuse reflectance) 3426 (s), 3011 (s), 2999 (s), 2888 (s), 2785 (s, b), 2740 (s, b), 2703 (s, b), 2649 (s, b), 2483 (s, b), 2483 (s, b), 2361 (s), 2354,2340, 2248,1638 (s), cm HRMS (FAB) [CALCD FOR C5HL2N2 +HI 101.] 1079, found [101.] 1080. [[A]] [25D] = [24] (c 1.00, water). Anal. Calcd for [C4H606.] [C5HL2N2C,] 43.20 ; H, 7.25 ; N, 11.19. Found: C, 41.25 ; H, 7.45 ; N, 10.71.

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

Reference£º
Patent; BIOVITRUM AB; WO2004/829; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

288251-85-4, tert-Butyl 4-(4-amino-2-cyanophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 21 3-(2,6-dichlorophenyl)-7-(methylthio)-2,3-dihydro-4H-pyrimido[5,4-e][1,3]oxazin-4-one (300 mg, 0.8767 mmol, 1.0 eq) in (10.0 mL) of 24 toluene was added 25 m-CPBA (376 mg, 2.1917 mmol, 2.5 eq) and allowed to stir at rt for 30 min followed by addition of 570 tert-butyl 4-(4-amino-2-cyanophenyl)piperazine-1-carboxylate (265 mg, 0.8767 mmol, 1 eq) and 27 DIPEA (452 mg, 3.506 mmol, 4.0 eq) and allowed to stir at rt for 12 h. The reaction mixture was diluted with water (50 mL) and extracted with EtOAc (2¡Á50 mL). The combined organic layers were washed with water (50 mL), brine (50 mL), dried over Na2SO4, concentrated and purified by flash chromatography (elution 0-35% 19 EtOAc in 20 Hexane) to afford the desired compound, 573 tert-butyl 4-(2-cyano-4-((3-(2,6-dichlorophenyl)-4-oxo-3,4-dihydro-2H-pyrimido[5,4-e][1,3]oxazin-7-yl)amino)phenyl)piperazine-1-carboxylate (150 mg, 28.68%) as an off white solid. (0600) LCMS: 596.2 [M+1]+, 288251-85-4

As the paragraph descriping shows that 288251-85-4 is playing an increasingly important role.

Reference£º
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (2019); 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.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: 1-BOC-3-Methylpiperazine (1.00 g) was combined with dichloromethane (10 mL), diisopropylethylamine (0.94 mL) and N-(benzyloxy-carbonyloxy)succinimide. The reaction was stirred at room temperature for 3 days and concentrated to dryness. The residue was diluted with ethyl acetate (20 mL) and washed with HCl (1 N in water, 3*5 mL), saturated aqueous sodium bicarbonate (3*5 mL) and brine (5 mL). The organic layer was dried over anhydrous magnesium sulfate, filtered and concentrated giving the desired benzyl carbamate. Yield=100percent, 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Millennium Pharmaceuticals, Inc.; US2003/153556; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics