Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

1-tert-butyl 2-methyl 4-(6-Bromo-7-chloro-2-methylquinazolin-4-yl)piperazine- 1,2-dicarboxylate To a solution of 6-bromo-4,7-dichloro-2-methylquinazoline (435 mg, 1.49 mmol) and 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (437 mg, 1.79 mmol in 1,4-dioxane (30 mL), DIEA (769 mg, 5.96 mmol) was added. The mixture was stirred at 80C for 1.5 h. The mixture was allowed to cool to RT and partitioned between water and ethyl acetate. The organic layer was washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash column chromatography on silica gel (5-50 % ethyl acetate/petroleum ether) to afford the desired product (224 mg, 30 % yield) as a yellow solid.

129799-15-1, As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; ARAXES PHARMA LLC; LI, Liansheng; FENG, Jun; WU, Tao; REN, Pingda; LIU, Yi; LIU, Yuan; LONG, Yun, Oliver; WO2015/54572; (2015); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.,70261-82-4

General procedure: A previously described method [19] was followed for the syntheses of 1-5, 7, 8, 10 and 20. Briefly, equimolar quantities of the amine and the acridine/quinoline were dissolved in ethanol, 2 drops of conc. HCl were added and the mixture refluxed for ca 24 h. On cooling, NaOH (1 M) or ammonia solution (25%) was added, followed by dichloromethane to extract the product. Alternatively, if the product precipitated out of solution on alkalinization, it was removed by filtration and purified by column chromatography.

As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference£º
Article; Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 2917 – 2929;,
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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.

Step 1: (S)-tert-butyl 4-(3,4-difluorophenyl)-2-methylpiperazine-1-carboxylate A mixture of 4-bromo-1,2-difluorobenzene (1 g, 5.18 mmol), (S)-tert-butyl 2-methylpiperazine-1-carboxylate (1.04 g, 5.18 mmol), t-BuONa (747 mg, 7.77 mmol), BINAP (40 mg, 0.06 mmol) and Pd2(dba)3 (20 mg, 0.02 mmol) in toluene (15 mL) was stirred at 80 C. for 3 hrs. The mixture was then purified by chromatography (silica, EtOAc/PE=1/8) to afford (S)-tert-butyl-4-(3,4-difluorophenyl)-2-methylpiperazine-1-carboxylate (921 mg, 2.95 mmol, 57%) as product. ESI-MS (EI+, m/z): 257.1 [M-55]+.

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

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); A1;,
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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.

109-07-9, Stage-2 : Preparation of 1-CYCLOPROPYL-7- 3-METHYLPIPERAZIN-1-YL)- 6-fluoro-8-methoxy-4-oxo-1, 4-DIHYDRO-3-QUINOLINE carboxylic acid boron difluoride chelate 100 g of Boron difluoride chelate derivative prepared as above in stage-1 is suspended in acetonitrile (800 ml), to that 2-methyl piperazine (44.0 g, 1. 5 mole EQUIV.) IS added and mixed for 15 min to obtain a clear solution. The reaction mass is maintained at 30C – 35C for 12 hrs followed by cooling TO-10C TO-5C. The reaction mass is maintained AT-10C TO-5C for 1 hr. The product is filtered and dried at 45C-50C to constant weight. Dry weight of the product : 116. 0 g (Yield : 93. 9 %).; Stage-2: Preparation of Gatifloxacin (Crude) The boron difluoride chelate derivative (100 g) prepared as above in stage-1 is suspended in acetonitrile (800 ml), 2-methyl piperazine (44 g, 1.5 mole equiv. ) is added and mixed for 15 min to obtain a clear solution. The reaction mass is maintained at 30C- 35C for 12 hrs. Removed the solvent by vacuum distillation. 20% Aq. ethanol (1000 ml) is added, raised the temperature and maintained at 75C to 80C for 2 hrs. The reaction mass is cooled, filtered to remove insolubles. The filtrate is distilled under vacuum to remove solvent completely. Fresh ethanol (250 ml) is added and distilled under vacuum at temperature below 50C. Fresh Ethanol (250 ml) is added to the residue and gradually cooled TO-10C TO-5C. The reaction mass is maintained AT-10C to-5C for 1 hr and filtered. The wet cake is washed with ethanol (30 ML) and dried at 45C-50C to constant weight. The dry weight of the Gatifloxacin is 73.5 g (Yield: 65.4 %)

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

Reference£º
Patent; MATRIX LABORATORIES LTD; WO2005/9970; (2005); A1;,
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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, 1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Triethylamine (3.83 mL) and di-tert-butoxydicarbonate (6.32 mL) were added at room temperature to piperazin-2-one (2.5 g) in a mixture of tetrahydrofuran (50 mL) and methanol (50 mL), followed by stirring for 4 hours. The reaction solvent was evaporated under reduced pressure. The residue was partitioned between water and ethyl acetate. The organic layer was sequentially washed with water and saturated brine. The aqueous layers obtained through washing were combined, and the combined layer was extracted with ethyl acetate. The organic layers were combined, followed by drying over magnesium sulfate anhydrate. After a filtration step, the solvent was evaporated under reduced pressure. Subsequently, ethyl acetate-hexane was added to the residue, followed by drying to solid, to thereby give 3-oxopiperazine-1-carboxylic acid tert-butyl ester (3.6 g, 72%). 1H-NMR(400MHz,CDCl3)delta:1.48(9H,s), 3.37-3.40(2H,m), 3.62-3.65(2H,m), 4.01(2H,s), 6.32(1H,br s). [Referential Example 40] 1-Ethyl-2-oxopiperazine hydrochloride [Show Image] 1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Piperazin-2-one (5.07 g) was dissolved in tetrahydrofuran (50 mL) and methanol (50 mL), and, at room temperature, triethylamine (7.76 mL) and di-tert-butyl dicarbonate (12.17 g) were added to the solution, followed by stirring for 4 hours. The reaction solvent was evaporated under reduced pressure, and diethyl ether was added to the residue. The precipitated solid was collected through filtration, to thereby give 3-oxopiperazine-1-carboxylic acid tert-butyl ester as a solid product (9.36 g, 92%). 1H-NMR(400MHz,DMSO-d6)delta:1.40(9H,s), 3.15(2H,br), 3.45(2H,br), 3.81(2H,br), 8.03(1H,br). ESI-MS m/z:201(M+H)+.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1762568; (2007); A1;,
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55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55121-99-8, A solution of 4-(4-methylpiperazine-1-carbonyl)aniline (1.03g, 4.56 mmol) in THF (50 mL) was cooled to 0C and LiAlH41 M in THF (14 mL, 14 mmol) was added dropwise. The mixture was let to warm to room temperature, and then refluxed for 3 h. After cooling to 0C Na2SO4.10H2O was added and the solution was filtered off. The solution was concentrated and purified by silica flash chromatography with 0 to 5% MeOH in DCM to give 4-[(4- methylpiperazin-1-yl)methyl]aniline (500 mg, 53% yield). MS found for C12H19N3 as (M+H)+ 206.3.

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PHARMACYCLICS LLC.; ATALLAH, Gordana, Babic; CHEN, Wei; JIA, Zhaozhong, J.; POZZAN, Alfonso; RAVEGLIA, Lucal, Francesco; ZANALETTI, Riccardo; (815 pag.)WO2016/196776; (2016); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.639068-43-2,tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,639068-43-2

tert-Butyl 3,5-dimethylpiperazin-1-carboxylate (200.0 mg, 0.93 mmol) and 37percent formaldehyde (440.0 muL, 5.56 mmol) were dissolved in MeOH (5.0 mL), and NaBH4 (172.6 mg, 5.56 mmol) was slowly added thereto and stirred at room temperature for 12 hours. Brine was poured into the reaction mixture, and it was extracted with DCM (30.0 mL). The organic layer was dried over anhydrous Na2SO4, filtered and then distilled under reduced pressure. The residue was purified column chromatography (DCM:MeOH=95:5) on silica to obtain yellow liquid compound of tert-butyl 3,4,5-trimethylpiperazin-1-carboxylate (57.0 mg, 27percent).

639068-43-2 tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 22219990, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; C&C RESEARCH LABORATORIES; Ho, Pil Su; Yoon, Dong Oh; Han, Sun Young; Lee, Won Il; Kim, Jung Sook; Park, Woul Seong; Ahn, Sung Oh; Kim, Hye Jung; US2014/315888; (2014); A1;,
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5464-12-0,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

1-(2-(4-bromo-3-fluorophenoxy)ethyl)-4-methylpiperazine: A flask was charged with 4-bromo-3-fluorophenol (5.00 g, 26 mmol) and triphenylphosphine (10.30 g, 39 mmol). Methylene chloride (120 mL) was added followed by 2-(4-methylpiperazin-1-yl)ethanol (4.61 g, 32 mmol) and the solution was stirred on an ice water bath to cool. After 5 minutes, diisopropyl azodicarboxylate (7.6 ml, 39.1 mmol) was added over 6 to 8 minutes. The reaction was left stirring on the cold bath to slowly warm to room temperature overnight. The reaction was concentrated and the residue purified by flash chromatography (25percent to 100percent EtOAc in hexanes) to provide the product as a colorless oil (2.62 g, 33percent).

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; Hangauer, David G.; US2006/160800; (2006); A1;,
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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.

tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate 4d (4 g,14.44 mmol) was dissolved in 40 ml of dry pyridine and stirred at0 C under inert atmosphere. Cinnamoyl chloride 6b (4.45 g,17.33 mmol) was dissolved in 20 ml dry DCM and added dropwiseto above stirred solution at 0 C. The reaction mixture was stirredfor 3 h. After completion of the reaction, the reaction mixture wasdiluted with 40 ml water and 60 ml ethyl acetate followed by 2 NHCl to make it acidic. The organic layer was separated and againwashed with 2 N HCl followed by saturated bicarbonate solution(2 50 ml) and brine solution. The organic layer was dried overanhydrous sodium sulfate and was evaporated under reducedpressure. The crude product was recrystallized from ethyl acetateand hexane to afford 4.52 g of 7l. Light yellow solid; Yield 69.33%;216e218 C (charred); IR (KBr pellets, cm1): 3425, 3105, 1666,1604, 1544, 1514, 1427, 1342, 1220, 1141, 991, 844; 1H NMR(400 MHz, CDCl3) d (ppm): 1.43 (9H, s, CH3), 3.10 (4H, t, J 3.79 Hz),3.62 (4H, t, J 3.76 Hz), 6.71 (1H, d, J 16.5 Hz, PheCH]CHe), 6.98(2H, d, J 7.2 Hz, AreH), 7.29e7.87 (4H, m, AreH), 7.89 (1H, d,J 16.5 Hz, PheCH]CHe), 8.23 (2H, d, J 7.0 Hz, AreH), 9.24 (1H,s, CONH); 13C NMR (100 MHz, CDCl3) d (ppm): 28.76, 49.41, 51.48,78.50, 112.10, 118.03, 121.31, 123.72, 126.08, 129.45, 141.79, 142.11,145.21, 147.29, 157.22, 167.52; HReMS m/z: 453.2067 (M 1)., 170911-92-9

The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Patel, Kavitkumar N.; Telvekar, Vikas N.; European Journal of Medicinal Chemistry; vol. 75; (2014); p. 43 – 56;,
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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

To a 25 mL flask was added TEA (177 mg, 244 ).ll, 1.75 mmol), tert-butyl piperazine-1-carboxylate (240 mg, 1.29 mmol), (bromomethyl)benzene (200 mg, 139 ).ll, 1.17 mmol) andDCM (4 mL). The colorless solution was stirred at rt for 3 hrs. The reaction mixture wasconcentrated to give a white solid. Then it was purified by silica gel column chromatography(eluted with EA/PE=15- 30% ), about 177 mg tert-butyl4-benzylpiperazine-1-carboxylate20 (Compound lOA) was obtained as a colorless oil. MS: calc’d 277 (M+Ht, measured 277(M+Ht, 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; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; WANG, Lisha; YUN, Hongying; ZHANG, Weixing; ZHU, Wei; ZHANG, Zhiwei; (69 pag.)WO2017/202704; (2017); A1;,
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