Month: May 2021

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, The 4-(2-hydroxyethyl)-l-methylpiperazin-2-one used as starting material was prepared as follows :-2-Bromoethanol (5.60 mL, 78.85 mmol) was added to 1 -methylpiperazin-2-one (1.80 g, 15.77 mmol) and potassium carbonate (6.54 g, 47.31 mmol) in THF (20 mL). The resulting mixture was stirred at 65¡ãC for 16 hours. The mixture was cooled to room temperature, fltered and the solvents evaporated to give crude product. The crude product was purified by flash silica chromatography, elution gradient 0 to 8percent MeOH in DCM. Pure fractions were evaporated to dryness to give 4-(2-hydroxyethyl)-l-methylpiperazin-2-one (1.870 g, 75.0percent). IH NMR (399.9 MHz, CDC13) delta 2.55 (2H, t), 2.71 (2H, t), 2.90 (3H, s), 3.15 (2H, s), 3.28 (2H, t), 3.60 (2H, t)

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BRADBURY, Robert, Hugh; RABOW, Alfred, Arthur; WO2010/131022; (2010); A1;,
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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

20.1: 3,3-Dimethyl-4-(1-phenyl-1H-[1,2,4]triazole-3-carbonyl)-piperazine-1-carboxylic acid tert-butyl ester A mixture of 420 mg (2.22 mmol) 1-phenyl-1H-[1,2,4]-triazole-3-carboxylic acid, 500 mg (2.22 mmol) 3,3-dimethyl-piperazine-1-carboxylic acid tert-butyl ester, 750 mg (2.22 mmol) TBTU and 500 muL (2.91 mmol) DIPEA in 5 mL DMF was stirred at RT for 2 h. The reaction mixture was poured into ice water. The precipitate was filtered off, taken up in EtOAc, dried over sodium sulfate, filtered and concentrated in vacuo. yield: 850 mg (99%) ESI-MS: m/z=386 (M+H)- Rt(HPLC): 1.20 min (method 23), 259808-67-8

259808-67-8 1-Boc-3,3-Dimethylpiperazine 22710387, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; US2013/158042; (2013); A1;,
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31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-1-carboxylic acid benzyl ester (8.00 g; 36.3 mmol), 2-fluoro-4-methyl-l-nitro;benzene (4.70 g; 30.3 mmol) and potassium carbonate (8.5 g; 61.5 mmol) were stirred 3 hours in 50 mL DMSO at 80¡ãC. The reaction mixture was cooled to room temperature and 250 mL water was added. The mixture was extracted with diethyl ether (2 x 250 mL). The organic phase was washed with water (100 mL), 1 N HC1 (2 x 100 mL), brine (2 x 100 mL), dried with MgSC>4 and concentrated in vacuo to give 10.5 g (29.5 mmol; 97.6 percent) 4-(5-methyl-2-nitro-phenyl)-piperazine-l-carboxylic acid benzyl ester.

31166-44-6, As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Patent; H. LUNDBECK A/S; WO2006/7843; (2006); A1;,
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Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2- (5-amino-2- (furan-2-yl) -8H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-8-yl) pentanoic acid (50 mg, 0.15 mmol) , 1- (2, 4-difluorophenyl) piperazine (32 mg, 0.16 mmol) , HATU (69 mg, 0.18 mmol) and DIEA (39 mg, 0.3 mmol) in DMF (5 mL) was stirred at rt for 2 hrs. The solution was added with water (5 mL) , extracted with ethyl acetate (10 mL) and washed with brine (10 mL) . The organic layer was dried, concentrated and purified by column chromatography (PE: EA = 1: 1) to get the desired product (49 mg, 64%) .1H NMR (400 MHz, DMSO-d6) delta 8.76 (s, 1H) , 7.95 (s, 1H) , 7.66 (br. s, 2H) , , 7.19-6.96 (m, 4H) , 6.74-6.73 (m, 1H) , 5.71-5.67 (m, 1H) , 3.78-3.65 (m, 4H) , 2.94-2.83 (m, 4H) , 2.19-1.99 (m, 2H) , 1.33-1.17 (m, 2H) , 0.92 (t, J = 8.0 Hz, 3H) ppm. MS: M/e 522 (M+1)+

115761-79-0, As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference£º
Patent; BEIGENE, LTD.; ZHANG, Guoliang; SUN, Hanzi; ZHOU, Changyou; (253 pag.)WO2020/20097; (2020); 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.187669-60-9,1-(4-(Methylsulfonyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 77; 4-{2-[4-(4-Methanesulfonylphenyl)piperazin-l-yl]ethylidene}piperidine-l- carboxylic acid tert-butyl ester; To a solution of 4-(2-hydroxyethylidene)piperidine-l-carboxylic acid tert-butyl ester (2.2g, 9.7mmol) in DCM (25mL) was added Et3N (2.02mL, 14.5mmol) and the reaction cooled to O0C. To this cooled mixture was added methanesulfonylchloride (0.98mL, 12.6mmol) dropwise. The reaction was stirred at O0C for 20 min then treated with saturated NaHCO3 solution. The two layers were separated and the organic layer washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by flash chromatography with 10% EtOAc / Hexane as eluent to afford 4-(2-chloroethylidene) piperidine-1-carboxylic acid tert-butyl ester and 4-vinyl-3,6-dihydro-2H-pyridine-l-carboxylic acid tert-butyl ester in a 1:1 ratio (0.95Og). The mixture was dissolved in DMF (5mL) and treated with TBAI (0.068g, 0.18mmol). This suspension was thus added to a preformed mixture of l-(4-methanesulfonylphenyl)piperazine (0.487g, 2.03mmol) and sodium hydride (0.1 Ig of a 60% dispersion in mineral oil, 2.77mmol) in DMF (5mL) at rt. The mixture was allowed to stir for 2h then treated with water. The aqueous was extracted with EtOAc and the combined organic layers washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by HPLC to afford the title compound (0.27g, 6%): RT = 2.41 min; m/z (ES+) = 450.2 [M+ H]+, 187669-60-9

As the paragraph descriping shows that 187669-60-9 is playing an increasingly important role.

Reference£º
Patent; PROSIDION LIMITED; WO2007/3964; (2007); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

A mixture of IV-II-l-c (28 mg, 0.1 mmol), 2-methoxy-4-(4-methylpiperazin-l- yl)benzenamine (22 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in 1.2 mL of t-BuOH was heated at 100 0C in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The dichloromethane was removed in vacuo and the resulting crude product was purified by preparative TLC with 3.5 N ammonia methanol solution and dichloromethane (1/25, v/v) to give the title compound IV-I (8 mg). 1H NMR (600 MHz, CDCl3) delta 8.32 (s, IH), 8.18 (d, J= 8.4 Hz, IH), 7.80 (dd, J= 1.8, 7.8 Hz, IH), 7.61 (s, IH), 7.51 (dd, J= 1.8, 7.8 Hz, IH), 7.40-7.34 (m, 2H), 6.54 (dd, J= 1.8, 8.4 Hz, IH), 6.52 (d, J= 1.8 Hz, IH), 3.85 (s, 3H), 3.55 (s, 3H), 3.23 (s, br, 4H), 2.69 (s, br, 4H), 2.43 (s, 3H). MS (ESI) m/z 463 (M+H)+.

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference£º
Patent; DANA FARBER CANCER INSTITUTE; GRAY, Nathanael, S.; DENG, Xianming; KWIATKOWSKI, Nicholas, Paul; WO2010/80712; (2010); 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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Under an argon atmosphere,2,6-Dibromo-3-nitropyridine (1.18 g, 4.20 mmol) was added to a solution ofWas dissolved in ethanol (20 mL).there Tert-butyl 4- (4-aminophenyl) piperazine-1-carboxylate (1.40 g, 5.04 mmol)Triethylamine (1.14 mL, 8.40 mmol) was added,And the mixture was stirred at room temperature for 18 hours.The resulting precipitate was collected by filtration,After washing with a small amount of ethanol and hexane,And dried to give the title compound (1.91 g, 95%)

170911-92-9, 170911-92-9 tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate 11011301, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; YAKULT HONSHA COMPANY LIMITED; ABE, ATSUHIRO; MAE, MASAYUKI; YAMAZAKI, RYUTA; SASAI, TOSHIO; NISHIYAMA, HIROYUKI; NAGAOKA, MASATO; MATSUZAKI, TAKESHI; (47 pag.)JP6023630; (2016); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

76003-29-7, In reference to the process disclosed in WO2012/031004, 2-nitro-5-bromopyridine (1.01 g, 5.0 mmol), tert-butyl 2-oxo-4-piperazinecarboxylate (1.00 g, 5.0 mmol, and cesium carbonate (3.26 g, 10.0 mmol) were suspended in 1,4-dioxane, and the suspension was bubbled with nitrogen gas for 30 minutes. To the suspension was added Xantphos (246 mg, 0.43 mmol) and tris(dibenzylideneacetone)dipalladium (229 mg, 0.25 mmol), and the mixture was stirred under reflux for two hours. The resultant reaction mixture was cooled to room temperature, and water and ethyl acetate were then added to the mixture, followed by filtration with Celite. The organic phase was separated from the filtrate, and the aqueous phase was extracted with ethyl acetate. The resultant organic phases were combined together and dried over anhydrous sodium sulfate, and the resultant solid was separated by filtration. The filtrate was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography to yield the title compound (1.08 g, 67%). 1H-NMR (CDCl3) delta: 8.67 (1H, d, J=2.4 Hz), 8.32 (1H, d, J=8.8 Hz), 8.15 (1H, dd, J=8.8, 2.4 Hz), 4.33 (2H, s), 3.93-3.83 (4H, m), 1.51 (9H, s)

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; Teijin Pharma Limited; MIZUNO, Tsuyoshi; SHIMADA, Tomohiro; UNOKI, Gen; EBISAWA, Masaru; TAKEUCHI, Susumu; MINAMIZONO, Kunio; SASAKI, Kosuke; YOKOSAKA, Takuya; IGARASHI, Junji; MARUYAMA, Akinobu; TAKAHASHI, Hiroshi; HORIE, Kyohei; SAKAI, Yuri; (447 pag.)EP3305785; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-Chloro-2-fluoro-l-nitrobenzene (0.5 g, 2.85 mmol), (S)-tert-b tyl 2-methylpiperazine-l- carboxylate (0.856 g, 4.27 mmol), and DIEA (0.995 mL, 5.70 mmol) were dissolved in DCM (20 mL). The reaction was stirred at reflux overnight. The mixture was concentrated and the residue was purified by chromatography (0 – 30% EtOAc hexanes) to give the title compound (1.0 g, 98%). LCMS mlz = 356.4 [M+H]+; NMR (400 M Hz, DMSO – d6) delta ppm 1.16 (d, 7 = 6.87 Hz, 3H), 1.41 (s, 9H), 2.76 – 2.90 (m, 1H), 2.97 – 3.23 (m, 4H), 3.66 – 3.79 (m, 1H), 4.12 – 4.23 (m, 1H), 7.18 (d, 7 = 8.65 Hz, 1H), 7.32 – 7.40 (m, 1H), 7.85 (d, 7 = 8.90 Hz, 1H)., 169447-70-5

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; ARENA PHARMACEUTICALS, INC.; TRAN, Thuy-Anh; KRAMER, Bryan Aubrey; SHIN, Young-Jun; WO2014/182673; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics

694499-26-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

General procedure: To amixture of substituted benzoic acid obtained in the last step (0.12 mmol) in 5mL DMF, 2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluroniumhexafluorophosphate (HATU, 0.18 mmol), ethyldiisopropylamine (DIPEA, 0.24 mmol)and 4-((4-methylpiperazin-1-yl)methyl)-3- (trifluoromethyl)aniline (0.1 mmol)was added. The resulting mixture was stirred at room temperature overnight. Thenthe reaction was extracted with ethyl acetate, washed with brine, dried overanhydrous Na2SO4, filtered and concentrated to give thecrude product, which was further purified by column chromatography to affordthe final compounds.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
Article; Han, Mei; Li, Shan; Ai, Jing; Sheng, Rong; Hu, Yongzhou; Hu, Youhong; Geng, Meiyu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 23; (2016); p. 5679 – 5684;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics