Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.112257-12-2,tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The 4-(2-bromo acetyl)-piperazine-1-carboxylic acid tert butyl ester (2.0 g, 6.5 mmol, 1 eq) was added to a stirred solution of N-[(5S)-{3-(3-fluoro-4-hydroxy-phenyl)}-2-oxo-oxazolidin-5-ylmethyl]-acetamide (step 4, example 1) (1.75 g, 6.5 mmol, 1 eq) and potassium carbonate (1.138 g, 9.75 mmol, 1.5 eq) in DMF (32 ml). The resulting mixture was heated to 80 C. and stirred for 30 min, then cooled and dichloromethane/methanol (100 ml, 9/1) added. The organic layer was then washed with water (2*10 ml) and saturated sodium chloride solution, and then dried over MgSO4. This was then filtered and the solvent is evaporated. The residue was purified by chromatography (dichloromethane/methanol 9/1) to give the product (1.72 g, 55%) as a brown solid.

112257-12-2, As the paragraph descriping shows that 112257-12-2 is playing an increasingly important role.

Reference£º
Patent; Morphochem Aktiengesellschaft Fuer Kombinatorische Chemie; Hubschwerlen, Christian; Specklin, Jean-Luc; Baeschlin, Daniel; Schmitt, Christine; Mueller, Stefan; Cappi, Michael W.; US9133213; (2015); B2;,
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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.

General procedure: 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoic acid (5) was synthesized by the method reported. [Nat Med. 2013, 19(2): 202-8] To a solution of compound 5 (100 mg, 0.175 mmol) in anhydrous dichloromethane, compound 4g (68 mg, 0.175 mmol), EDCI (167 mg, 0.875 mmol) and DMAP (25.6 mg, 0.21 mmol) were added. Afterwards, the mixture solution was stirred for 24 h at room temperature. Completion of the reaction was confirmed by TCL. The reaction mixture was washed with HCl (1 M), NaHCO3 saturated solution and brine, concentrated and purified to afford 6g (160 mg, 85% yield) as a yellow solid.

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

Reference£º
Article; Zhou, Ruolan; Fang, Shaoyu; Zhang, Minmin; Zhang, Qingsen; Hu, Jian; Wang, Mingping; Wang, Chongqing; Zhu, Ju; Shen, Aijun; Chen, Xin; Zheng, Canhui; Bioorganic and Medicinal Chemistry Letters; vol. 29; 3; (2019); p. 349 – 352;,
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Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 3 (4-Cyclopentyl-piperazin-1-yl)-{3-[1-methyl-pyrrolidin-(2Z)-ylidene]-3H-indol-6-yl}-methanone A mixture of 0.4 g (1.43 mmol) 3-[1-Methyl-pyrrolidin-(2Z)-ylidene]-3H-indole-6-carboxylic acid; hydrochloride, 0.53 g (1.7 mmol) TBTU, 1.11 g (8.7 mmol) DIPEA and 0.27 g (1.73 mmol) 1-cyclopentyl-piperazine in 30 mL DMF was stirred at room temperature for 16 h. After evaporation of all volatiles acetone, THF and Na2CO3 (aq. 10%) was added and extracted with THF and acetone. The combined organic layers were washed with NaCl aq. sat., dried with Na2SO4 and evaporated to dryness. Isolute and DCM were added and again evaporated to dryness. The residue was purified by flash column chromatography on silica eluding with a mixture formed from DCM, MeOH and NH3 aq. to yield after evaporation of the combined product fractions and subsequent crystallization from ethyl acetate and diethyl ether 209 mg (38%) of the title compound as white solid. MS (m/e): 379.3 (MH+)., 21043-40-3

As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference£º
Patent; Nettekoven, Matthias; Roche, Olivier; US2008/32976; (2008); A1;,
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57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1-15 (3.0 g, 14.99 mmcl), 1-Boc-piperizine(3.33 g, 17.99 mmcl) and Cs2003 (9.68 g, 29.98 mci) in DMSO(60 ml) was stirred at 12000 for 1 hour. The reaction mixture was diluted with water (100 mL) and extracted with diethyl ether (100 ml x 3) . The organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure to give thedesired product 1-16 (2.5 g, 44%) as yellow solid which wasused in the next step without purification; LCMS: m/z 312 [MtBu+1], 57260-71-6

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; KOUL, Summon; KURHADE, Suresh; NAIK, Keshav; SALUNKHE, Videsh; KULKARNI, Rakesh; PARDESHI, Vishwajeet; BHUNIYA, Debnath; KULKARNI, Bheemashankar; MOOKHTIAR, Kasim Abbaas; (274 pag.)WO2017/38909; (2017); A1;,
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171504-98-6, Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step P: di-tert-butyl 2-(hydroxymethyl)piperazine-l,4-dicarboxylate 27. To a solution of 1 ,4- di-tert-butyl 2-methyl piperazine-l ,2,4-tricarboxylate (26; 2 g, 56 mmol) in ethanol (10 mL) was added CaCl2 (5 g, 45 mmol) at 0C, followed by NaBFL (1.1 g, 28 mmol) in two portions. The reaction mixture was warmed to room temperature and stirred for 1.5 h. After cooling to 0C, the mixture was quenched with aq. citric acid solution (6 g citric acid in 50 mL of water). The resulting mixture was then extracted with ethyl acetate (200 mL), and the organic layer was washed with brine, dried over anhy. Na2SC>4, filtered, and concentrated in vacuo to give 1.8 g of the crude title compound as a white solid.

171504-98-6, As the paragraph descriping shows that 171504-98-6 is playing an increasingly important role.

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;,
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109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: 2-Methylpiperazine (5.03 g) was dissolved in dichloromethane (200 mL) and a solution of di-tert-butyl-dicarbonate (10.96 g) in dichloromethane (100 mL) was added over 2.5 hours. The reaction was stirred at room temperature for 24 hours and concentrated to dryness giving 1-BOC-3-methylpiperazine. Yield=100%, 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1214196-85-6,1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of 1 g rac-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (9, 4.3 mmoles) in 20 mL of anhydrous N,N-dimethylformamide was added 1.7g (12.3 mmoles) of granular potassium carbonate. The slurry wasstirred for 1 hour, and then 1.3 mL (11 mmoles) of benzyl bromide was added and the mixture stirred for an additional 40 hours at room temperature. The reaction mixture was then diluted with water and extracted with ethyl ether. The organic layer was separated and washed with brine (NaCl(aq.)) solution twice. The organic layer was then dried over anhydrous sodium sulfate. Filtration, solvent removal and column chromatography (Hexanes:Ethylacetate gradient) gave 1.49 g of a clear viscous oil (83% yield), which solidified upon standing.

1214196-85-6, The synthetic route of 1214196-85-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Zhao, Huanyu; Prosser, Anthony R.; Liotta, Dennis C.; Wilson, Lawrence J.; Bioorganic and Medicinal Chemistry Letters; vol. 25; 21; (2015); p. 4950 – 4955;,
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

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

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
Piperazines – an overview | ScienceDirect Topics