Month: October 2020

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

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 46: 1,1-dimethylethyl (3S)-3-(hydroxymethyl)-4-(trifluoroacetyl)-1-piperazinecarboxylate 1,1-dimethylethyl (3S)-3-(hydroxymethyl)-1-piperazinecarboxylate (Commercial) (350 mg, 1.618 mmol) was dissolved in Dichloromethane (DCM) (10 ml) and cooled in an ice bath under nitrogen. Triethylamine (0.564 ml, 4.05 mmol) was added followed by the careful addition of trifluoroacetic anhydride (0.571 ml, 4.05 mmol). After ?10 mins, the ice bath was removed and the reaction was allowed to warm to room temperature and stirred for 3 hours. The reaction was washed with water. The aqueous was extracted with DCM. The combined organics were washed with water, dried using a hydrophobic frit and evaporated in vacuo to give a pale yellow oil (0.69 g) LCMS (Method B): Rt=0.45 min, MH+=245, 314741-40-7

The synthetic route of 314741-40-7 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.; US2014/5188; (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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A 100 mL round-bottom flask was charged with 2-chloro-4-(morpholin-4- yl)benzaldehyde (0.800 g, 3.54 mmol, 1.00 equiv), tert-butyl (2S)-2-methylpiperazine-l- carboxylate (0.783 g, 3.91 mmol, 1.10 equiv) , 1,2-dichloroethane (20 mL). The mixture was stirred for 30 min at room temperature. Sodium triacetoxyborohydride (2.26 g, 10.7 mmol, 3.00 equiv) was added. The resulting solution was stirred overnight at room temperature, diluted with ]0 (30 mL), extracted with dichloromethane (3 x 30 mL) and the organic layers were combined, dried over Na2S04, filtered and concentrated under reduced pressure. The residue was chromatographed on a silia gel column with ethyl acetate/petroleum ether (25/75) to provide 1.20 g (74% yield) of tert-butyl (2S)-4-[[2-chloro-4-(morpholin-4- yl)phenyl]methyl]-2-methylpiperazine-l-carboxylate as a white solid. LCMS (ESI, m/z): 410 [M+H]+., 169447-70-5

Big data shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; ABIDE THERAPEUTICS; THE SCRIPPS RESEARCH INSTITUTE; CISAR, Justin, S.; GRICE, Chery, A.; JONES, Todd, K.; NIPHAKIS, Micah, J.; CHANG, Jae, Won; LUM, Kenneth, M.; CRAVATT, Benjamin, F.; WO2013/103973; (2013); 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.954388-33-1,(R)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.,954388-33-1

Step 1. 1 -benzyl 4-tert-butyl f2R)-2-[(2.2,2-trifluoroethyl)carbamoyl]piperazine-L4- dicarboxylateA solution of (R)~N-4-BOC-N-l-CBZ-piperazine carboxylic acid (4.0 g, 11 mmol), 2,2,2-trifluoroethyiamine hydrochloride (1.78 g, 13 mmol), EDC (2.74 g, 14 mmol), HOBt (1.68 g, 11 mmol) and Hunig’s base (5.75 mL, 33 mmol) in DCM (100 mL) was stirred at ambient temperature for 18 h. The reaction mixture was washed with aqueous 5% sodium bicarbonate (100 mL) and brine. The organic layer was dried over sodium sulfate, filter and concentrated in vacuo. The residue was purified by silica gel chromatography, eluting with a gradient of 5 – 70 % ethyl acetate in hexane, to afford the title compound as white foam. MS APCI: [M + Na]+ m/z – 468.0.

954388-33-1 (R)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 6558854, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; CASH, Brandon; FISCHER, Christian; GARCIA, Yudith; JUNG, Joon; KATZ, Jason; KIM, June; RIVKIN, Alexey; SCHELL, Adam; SIU, Tony; WITTER, David; ZHOU, Hua; WO2011/137022; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics