Heterocyclic Building Blocks-piperazine

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,630125-91-6

A mixture of starting material (29 mg, 0.1 mmol), 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (29 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in t-BuOH (1.5 mL) was heated at 100 C. in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The solvent was removed in vacuo and the residue was purified by HPLC to afford the title compound (26.3 mg).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; Gray, Nathanael S.; Waller, David; Choi, Hwan Guen; Wang, Jinhua; Deng, Xianming; (104 pag.)US2016/24115; (2016); 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.197638-83-8,1-Boc-4-(4-Formylphenyl)piperazine,as a common compound, the synthetic route is as follows.

tert-Butyl 4-(4-(6-chloro-7-(4-((2-methylthiazol-4-yl)methyl)piperazin-1-yl)-3H- imidazo[4,5-/fc>]pyridin-2-yl)phenyl)piperazine-1-carboxylateTo a mixture of 5-chloro-4-(4-((2-methylthiazol-4-yl)methyl)piperazin-1-yl)-3- nitropyridin-2-amine (0.100 g, 0.27 mmol, 1 eq), EtOH (4.73 mL) and DMF (0.63 mL), te/Y-butyl-4-(4-formylphenyl)tetrahydro-1-(2H)pyrazine carboxylate (0.087 g, 0.3 mmol, 1.1 eq) was added followed by a freshly prepared aqueous solution of Na2S2O4 (1 M; 0.82 ml_, 0.82 mmol). The reaction mixture was heated at 85C for 24 h, then allowed to cool to room temperature and diluted with DCM and a few drops of aqueous NH3 until complete dissolution was observed. This solution was deposited on two preparative silica TLC plates and eluted with DCM/MeOH (v/v; 94:6). The title compound was obtained after trituration with diethyl ether as a off-white solid (0.025 g, 15%); 1H-NMR (500Mz, DMSO-c/6): delta 1.43 (s, 9H, C(CH3)3), 2.63-2.69 (m, 7H1 piperazine N(CH2)2 and thiazole Me), (piperazine N(CH2)2 masked under water or DMSO peak), 3.45-3.51 (m, 4H, piperazine N(CH2)2), 3.63 (s, 2H, NCH2), 3.65-3.71 (m, 4H, piperazine N(CH2J2), 7.07 (d, J = 9.0 Hz, 2H1 ArH, C6H4), 7.31 (s, 1 H, thiazole 5-H)1 8.00-8.06 (m, 3H, ArH, C6H4 and imidazo[4,5-iotab]pyridine 5-H)1 13.18 (br s, 1 H, imidazo[4,5-iotab]pyridine N-H); LC (Method B) – MS (ESI, m/z) 3.93 min – 609/611 [(M+H)+, Cl isotopic pattern]; ESI-HRMS: Found: 609.2648, calculated for C30H38CIN8O2S (M+H)+: 609.2521.

197638-83-8, 197638-83-8 1-Boc-4-(4-Formylphenyl)piperazine 2795509, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CHROMA THERAPEUTICS LTD.; WO2009/1021; (2008); 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.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

To a flask containing a solution of 1 (0.25g, 1 mmol), 4-(4-ethylpiperazin-l- yl)aniline (0.23g, 1.1 mmol), cesium carbonate (0.5g, 1.5 mmol), racemic-2,2′- bis(diphenylphosphino)-l,l’-binaphthyl (95mg, 0.15 mmol) in N,N-dimethylacetamide (5mL) purged with N2 was added tris(dibenzylideneacetone)dipalladium(0) (0.14g, 0.15 mmol). This reaction was heated to 90 0C for 16 h under N2. At this time the reaction was concentrated and the residue was purified via silica gel column chromatography. The column was eluted with ethyl acetate to remove the impurities and then with 85:10:5 (ethyl acetate/methanol/7M ammonia in methanol) to elute the desired product. The solid obtained was sonicated first in acetone (5mL) and then in ether (1OmL) to yield intermediate 2 (0,23g, 48% yield) as a yellow solid. LCMS: m/z 417 (MH+). To a flask containing 2 (0.23g, 0.45 mmol) was added 4N HCl in dioxane (5mL) and the solution was heated at 50 0C for 4 h. To the cooled solution was added a 2N aqueous solution of sodium hydroxide (1OmL) and the resulting precipitate was filtered and dried to yield 3 (0.2g, 99% yield) as a yellow solid. LCMS: m/z 375 (M+H)+. To a flask with 3 (0.3g, 0.8 mmol), phenylacetic acid (0.125mL, 1 mmol), triethylamine (0.97mL, 7 mmol), and DMF (5mL) was added O-(7-azabenzotriazole- l-yO-N.iV.JV’.N’-tetramethyluronium hexafluorophosphate (HATU) (0.46g, 1.2 mmol). The reaction mixture was stirred at ambient temperature for 1 h then diluted with 5% aqueous solution of lithium chloride (10OmL) and extracted with ethyl acetate (3 x 5OmL). The combined organic layers were washed with an aqueous 5% sodium bicarbonate solution, a saturated aqueous solution of sodium chloride, dried over anhydrous sodium sulfate, filtered and concentrated. The residue obtained was purified by silica gel column chromatography (98:2 ethylacetate/methanol) to provide Compound 329 (0.25g, 63% yield) as an off-white solid., 115619-01-7

The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EXELIXIS, INC.; WO2007/89768; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

181955-79-3, 1,4-Di-Boc-piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step O:1,4-di-tert-butyl 2-methyl iperazine-l,2,4-tricarboxylate (26; Rb=Me). To a mixture of 1 ,4- bis(ieri-butoxycarbonyl)-piperazine-2-carboxylic acid (25; 3.6 g, 1 1 mmol) in DMF (10 mL) was added K2C03 (2 g, 18 mmol). The resulting suspension was cooled to 0C and treated with iodomethane (1.5 mL, 12 mmol). The mixture was then allowed to warm to room temperature, stirred for 6 hours. After quenched with water (200 mL), the mixture was extracted with ethyl acetate (100 mL), and the organic layer was washed with brine, dried over anhy. Na2SC>4, filtered, and concentrated in vacuo to afford 3.6 g of the title compound as a white solid.

181955-79-3, The synthetic route of 181955-79-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AGIOS PHARMACEUTICALS, INC.; CAO, Sheldon; POPOVICI-MULLER, Janeta; SALITURO, Francesco G.; SAUNDERS, Jeffrey; TAN, Xuefei; TRAVINS, Jeremy; YAN, Shunqi; YE, Zhixiong; WO2012/171506; (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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

22.8) 5-Chloro-thiophene-2-carboxylic acid [(S)-3-(4-cyclopropyl-piperazin-1-yl)-2-(2- methyl-3-pyridin-3-yl-benzenesulfonylamino)-3-oxo-propyl]-amide dihydrochloride: Intermediate 78 (202 mg, 0.42 mmol) was dissolved in 10 ml DCM and N-cyclopropyl piperazine (105 mg, 0.84 mmol) was added followed by DIPEA (0.29 ml, 1.68 mmol) and TBTU (202 mg, 0.63 mmol). After stirring for 1 h at RT the solution was evaporated to dryness and purified by silica gel chromatography (Elution with DCM/methanol from 0 to 10% of methanol). The solid obtained after evaporation of the solvents was dissolved in DCM, HCI 2M in Et2O (5 ml) was added and the solvents were evaporated. Yield: 163 mg, 59 %. MS (ES+): m/e = 588.

20327-23-5, The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SANOFI-AVENTIS; WO2009/103440; (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.129722-25-4,7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one,as a common compound, the synthetic route is as follows.

General procedure: To a solution of dehydro-Aripiprazole (1.0 g, 2.24 mmol) in 2-methyltetrahydroffiran (25 mE) was added silver carbonate (0.864 g, 3.13 mmol) and iodomethyl octanoate (0.764 g, 2.68 mmol) at room temperature. The reaction was stirred for5 days. The reaction was quenched with H20 (30 mE) and filtered through celite. The reaction was extracted with ethyl acetate (3×20 mE), washed with 5% w/v sodium sulfite solution (15 mE), brine (20 mE), dried over MgSO4 and concentrated. The product was purified by column chromatography on silica eluting with 0-70% ethyl acetate in heptane to provide Compound 1206 (0.602 g) as a pale orange oil.?H-NMR (300 MHz, CDC13) oe 7.95 (1H, d), 7.60 (1H, d),7.21 (1H, m), 7.14 (2H, m), 7.07 (1H, dd), 6.95 (1H, m), 6.79(1H, d), 6.24 (2H, s), 4.12 (2H, m), 3.09 (4H, m), 2.68 (4H,m), 2.54 (2H, m), 2.36 (2H, t), 1.90 (2H, m), 1.77 (2H, m),1.61 (4H, m), 1.23 (6H, m), 0.83 (3H, t). [M+H]=602.2, 129722-25-4

The synthetic route of 129722-25-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Alkermes Pharma Ireland Limited; Blumberg, Laura Cook; Remenar, Julius F.; Almarsson, Orn; Zeidan, Tarek A.; US9102618; (2015); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

27561-62-2, Cyclohexyl(piperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-[4-(4-Cyclohexanecarbonyl-piperazine-1-carhonyl)-pyridin-2-ylmethyl-2H-phthalazin-1-one (5)To a stirred solution of 2-(4-oxo-3,4-dihydro-phthalazin-1-ylmethyl)-isonicotinic acid (iva)(0.25g, 0.89mol) in diemthylacetamide (2mL) was added cyclohexyl-piperazin-1-yl-methanone (0.20g, LOmmol) followed by HBTU (0.38g, LOmmol) and diisopropyl ethyl amine (0.35mL, 20.0 mmol) and stirred. The reaction mixture was then concentrated in vacuo and resulting oil subjected to flash chromatography eluent 9:1 EtOAc / MeOH. (rf of 0.3) The titledcompound was isolated as a white solid. Single peak in LC-MS analysis, (0.18g, 56%); m/z (LC-MS, ESP), RT=4.07mins, (M+H)=460; 1H NMR (300 MHz) 12.57 (1H, S -NH), 8.56 (1H, d, J 5.1 Hz), 8.26 (1H, dd, J 1.5, 8.1Hz), 7.95- 7.80 (3H, m), 7.38 (1H, S), 7.25 (1H, d, J 5.7Hz), 4.51 (2H, S), 3.56-3.17 (8H, m), 2.58 (1H, m), 1.71-1.61 (5H, m), 1.38-1.22 (5H, m).

27561-62-2, The synthetic route of 27561-62-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KUDOS PHARMACEUTICALS LIMITED; WO2006/21801; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, A solution of l-methylpiperazin-2-one (cas: 5625-67-2, 1 g, 9.99 mmol), tert- butyl (2-bromoethyl)carbamate (cas: 39684-80-5, 2 g, 0.9 equiv.) in anhydrous DMF (15 mL) was added K2CO3 (8.28 g, 6.0 equiv.). The reaction mixture was stirred for 8 hours at ambient temperature. Once LC-MS analysis indicated reaction completion, the reaction was quenched with H20 (20 mL) and the aqueous phase was extracted with EtO Ac (20 mL x 3). The combined organic extracts was concentrated under reduced pressure to give the crude product. The crude product was purified by silica gel chromatography (Petroleum ether: EtO Ac = 1 : 10) to provide carbamate 1-333 as a pale oil (0.65 g, 22%). MS (ESI, pos. ion) m/z: 258(M+l).

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CARMOT THERAPEUTICS, INC.; ENQUIST, Johan; KRISHNAN, Shyam; ATWAL, Suman; ERLANSON, Daniel; FUCINI, Raymond V.; HANSEN, Stig; SAWAYAMA, Andrew; SETHOFER, Steven; (719 pag.)WO2019/183577; (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.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

Compound 6 (0.20 g, 1.02 mmol), 1-methyl-3-phenylpiperazine (0.22 g, 1.22 mmol) obtained in the above,Ethyl-3- (3-dimethylaminopropyl) carbodiimide (0.39 g, 2.04 mmol),1-hydroxybenzotriazole (0.13 g, 1.02 mmol), 1-hydroxybenzotriazoleN, N-diisopropylethylamine (0.18 mL, 1.02 mmol) and N, N-diisopropylethylamineThe mixture of 4 mL of solvent DMF was mixed well at the same time while performing a microwave irradiation (Biotage Initiator) at 120 ¡ã C for 3 hours. The mixture was concentrated under reduced pressure, And purified by MPLC (Biotage SNAP Cartridge KP-C18-HS column) to obtain Compound 1 at a yield of 27percent. Rf = 0.32 (8: 2 ethyl acetate: hexane)., 5271-27-2

As the paragraph descriping shows that 5271-27-2 is playing an increasingly important role.

Reference£º
Patent; Keimyung University; Industrial Cooperation Foundation CHONBUK NATIONAL UNIVERSITY; Seo Yeong-ho; Kim Won-il; Kim Beom-seok; Cho Ho-seong; Lee Sang-myeong; (12 pag.)KR101789269; (2017); 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.68104-63-2,4-(Piperazin-1-yl)benzonitrile,as a common compound, the synthetic route is as follows.,68104-63-2

Step B 4-(4-ethyl)piperazinylbenzonitrile Under a nitrogen atmosphere, a stirred solution of 3.16 grams (0.017 mole) of 4-piperazinylbenzonitrile, 2.0 mL (0.025 mole) of iodoethane (available from Aldritch Chemical Company), and 7.1 mL (0.051 mole) of triethylamine in 50 mL of THF was heated at reflux for about three hours. At the conclusion of this period, the reaction mixture was allowed to cool to ambient temperature and 100 mL of water was added. The resulting solution was extracted with two 50 mL portions of diethyl ether. The combined extracts were washed with 100 mL portion of water, dried with sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure, yielding 3,2 grams of crude product. The crude product was purified by column chromatography on silica gel, yielding 2.9 grams of tilte compound. The NMR spectrum was consistent with the proposed structure.

68104-63-2 4-(Piperazin-1-yl)benzonitrile 2733995, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Theodoridis, George; Barron, Edward; Cohen, Daniel H.; Crawford, Ellen M.; Cullen, Thomas G.; Qi, Hongyan; Rowley, Elizabeth; Ali, Syed F.; Yeager, Walter H.; Duggan, Christina B.; US2002/183342; (2002); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics