Heterocyclic Building Blocks-piperazine

20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 2.07 g (10.0 mmol) of the product prepared in step 14.1 in 30 mL of acetonitrile are added 5.99 mL (35.0 mmol) of diispropylethylamine and then 2.09 g (10.5 mmol) of finely ground N-cyclopropylpiperazine (supplier). The reaction mixture is heated at 100 C. for 1 hour 30 minutes, cooled and concentrated under vacuum. The residue is taken up in 75 mL of ethyl acetate and washed with saturated aqueous NaHCO3 solution and with saturated aqueous NaCl solution. The organic phase is dried over Na2SO4, filtered and concentrated under vacuum. After triturating in cyclohexane, the solid is drained by suction and dried in an oven under vacuum. 2.33 g of the expected product are obtained in the form of a yellow solid, which is used as obtained in the following step. Yield=74.5%.

20327-23-5, 20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SANOFI; US2012/277220; (2012); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.859518-35-7,tert-Butyl 3-cyanopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

859518-35-7, A solution of tert-butyl 3-cyanopiperazine-1-carboxylate, prepared as described in the previous step, (10 g, 0.047 mol) and 2-(2-hydroxyethoxy)acetaldehyde (14.8 g) (see: Bodin, A., Contact Dermatitis, 2001, 44:207) in dichloromethane was treated with formic acid (12.7 g), and the reaction mixture was stirred at room temperature overnight. Sodium cyanoborohydride (7.2 g, 0.118 mol) was added in portions. The reaction mixture was stirred at room temperature for 3 hours followed by the addition of water and extraction with dichloromethane. The organic layer was washed with brine, dried over sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography to provide the product. 1H NMR: (CDCl3, 400 MHz): delta (ppm) 4.15 (s, 1H), 3.69-3.63 (m, 4H), 3.58 (d, J=4.4 Hz, 2H), 3.47-3.44 (m, 4H), 2.61 (d, J=5.2 Hz, 2H), 2.51-2.48 (m, 4H), 1.43 (s, 9H).

The synthetic route of 859518-35-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Janssen Pharmaceutica NV; Hryhorenko, Eric; Sankaran, Banumathi; DeCory, Thomas R.; Tubbs, Theresa; Colt, Linda; Remmerie, Bart M.; Salter, Rhys; Donahue, Matthew Garrett; Gong, Yong; (53 pag.)US9850318; (2017); B2;,
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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

EXAMPLE IX; Synthesis of Piperazine derivatives; Chemical Formula: C16H2iN3Oe Chemical Formula: C12H15N304 Molecular Weight: 130.15 Molecular Weight: 351.35 Molecular Weight: 265.27a: Boc-ON, NaOH, Dioxaneb: 2-flouronitrobenzene, K2C03, DMSOc: SOCI2, methanol, reflux, 2hrsd: Fmoc-NCS, CH2CI2/DMF; 20% piperidine in methanole: appropriate bromoacetophenonef: 1 N NaOH, Dioxane, reflux, 0.5hrs4-(feri-butoxycarbonyl)piperazine-2-carboxylic acid; [191] 4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid : To a solution of 2-piperazine- carboxylic acid dihydrochloride (1.0 g, 4.92 mmol) in 20 mL of water/dioxane 1 : 1, NaOH 6N was added to adjust the pH to 11. A solution of BOC-ON (1.34 g, 5.41 mmol) in dioxane (5 mL) was then added dropwise, while maintaining the pH=l 1 during the addition and the resulting solution was stirred overnight at room temperature. Another 0.134 g of BOC-ON were added and the reaction mixture was stirred for 2h. The solvent was evaporated under reduced pressure and the residue was diluted with diethyl ether/water (60 mL). The phases were separated and the pH of the aqueous layer was adjusted to 7 by slow addition of HC1 IN. Evaporation of water under reduced pressure afforded the title compound as a white solid which was dried in a vacuum oven at 50 C and used without further purification for the next step., 3022-15-9

3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PRESIDENT AND FELLOWS OF HARVARD COLLEGE; CHOREV, Michael; AKTAS, Bertal Huseyin; HALPERIN, Jose A.; WAGNER, Gerhard; WO2012/6068; (2012); A2;,
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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,57260-71-6

Synthesis of 4-(4-formyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (1). A mixture of 4-(tert-butyl-l -piperazinecarboxylate (556 mg, 3.0 mmol), 4- fluoro-benzaldehyde (315 mul, 3.0 mmol) and K2CO3 (514 mg, 3.7 mmol) in DMF (5 ml) was stirred at ambient temperature overnight. Reaction was diluted with water (30 ml) and extracted with EtOAc (50 ml x 2). Organic layer was washed with water (20 ml), 1 M aq. HCl (20 ml), water (20 ml x 2) and brine (20 ml) and dried over MgSO4 (anh.). Solvent was evaporated in vacuum. Residue was triturated with hexane. Formed precipitate was filtrated and dried in vacuum overnight to provide target compound (1) (342 mg, 39%) as off-white solid. LC-MS [M+H] 291.2 (C16H22N2O3+H, requires 291.38).

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ACHAOGEN, INC.; WO2008/154642; (2008); A2;,
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Piperazines – an overview | ScienceDirect Topics

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 0.342 g of 4-(4-ethyl-piperazine-1yl)phenylamine (4d;0.00167 mol) in a dry round bottom flask was added 10 mL of 98%ethanol. The mixture was stirred at room temperature till completedissolution. Then 0.350 g of ethyl 2,4-dioxo-6-phenylcyclohexanecarboxylate(E164; previously synthesized in our lab)23 was added.The reaction mixture was refluxed for about 6 h. The reaction wasmonitored by thin layer chromatography (dichloromethane: methanol85/15). After 6 h, the heat was turned off and reaction continued to stirovernight. After reaction was completed, the reaction was adsorbed ona silica gel and purified by automated flash chromatography (dichloromethane:methanol 75/25) to yield a dark orange solid (0.7059 g,94.9%). 1H NMR (300 MHz, d- CDCl3): delta (ppm) 0.992-1.040 (t, 3H),1.115-1.163 (t, 3H), 2.474-2.498 (q, 2H), 2.600-2.633 (t, 4H),3.203-3.237 (t, 4H), 3.237 (d, 1H), 3.622-3.663 (m, 1H), 4.008-4.037(q, 2H), 5.482 (s, 1H), 6.876-6.906 (d, 2H), 7.052-7.082 (d, 2H),7.297-7.326 (m, 5H). HRMS (ESI): m/z, Calcd. for C27H33N3O3[M+H]+: 448.2589, found 448.2635

115619-01-7, 115619-01-7 4-(4-Ethylpiperazin-1-yl)phenylamine 936738, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Ghoneim, Ola M.; Bill, Ashley; Dhuguru, Jyothi; Szollosi, Doreen E.; Edafiogho, Ivan O.; Bioorganic and Medicinal Chemistry; vol. 26; 14; (2018); p. 3890 – 3898;,
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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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of 2-chloro-5-nitropyridine (2.5g, 15.7mmol) in THF (25mL), are added1 -isopropylpiperazine (2.01g, 15.7mmol) and K2CO3 (3.25g, 23.6mmol). The reaction mixture is stirred at 5O0C for 4 hours and then at 7O0C overnight. The solvent is removed in vacuo and the resultant orange solid is triturated using 10:1 petroleum ether-diethyl ether. The isolated compound (3.7g, 94percent) is used in the next step without further purification.

4318-42-7, As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference£º
Patent; GALAPAGOS N.V.; WO2007/138072; (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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

A solution of anhydrous piperazine (1, 9.4 g, 0.11 mol) and piperazine dihydrochloride (2, 31.8 g, 0.20 mol) in ethanol (80 mL) was placed in a three-necked flask equipped with a magnetic stir bar and reflux condenser and was heated with vigorous stirring at 65 C for 3 h. Then benzyl chloride (12.6 g, 0.10 mol) was added dropwise over a period of 45 min to the reaction mixture, which was then refluxed for another 2h. The progress of the reaction was monitored by TLC. The mixture was cooled and the precipitated piperazine dihydrochloride (2) was recovered. The combined filtrate was concentrated under reduced pressure to give the N-benzylpiperazine hydrochloride, which was then treated with 4 M NaOH to pH > 12. The aqueous layer of crude N-benzylpiperazine was extracted with CHCl3 (3 ¡Á 50 mL). The combined organic extracts were dried over Na2SO4 and concentrated under reduced pressure. The crude product was purified by flash column chromatography on silica gel (1:5 MeOH-CH2Cl2) to give 4: Yield 18.3 g (95%); 1H NMR (500 MHz, CDCl3): delta 7.34-7.28 (m, 5H),3.57 (s, 2H), 3.23 (s, 4H), 2.77 (s, 4H); MS (ESI) m/z: 177 [M + H]+.Spectroscopic data are according to the literature.13, 142-64-3

142-64-3 Piperazine Dihydrochloride 8893, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Hu, Xiao; Chen, Hui; Wu, Wei-Jun; Wang, Wen-Ling; Wang, Jin; Journal of Chemical Research; vol. 40; 9; (2016); p. 519 – 520;,
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Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-bromo-N-[4-(5-cyano-7-methyl-l,3-benzoxazole-2-yl)phenyl]acetamide (0.025 g, 0.068 mmol, from Step A) in dimethylformamide (0.5 mL) was added l-(4- trifluoromethylphenyl)piperazine (0.016g, 0.068mmol) followed by triethylamine (0.019ml, 0.136mmol) at 6O0C. The solution was stirred at 6O0C for 1 hr. After concentration under reduced pressure the residue was purified on a 1000 micron preparative thin layer chromatography plate eluting with 5% methanol in dichloromethane to give the title compound as a solid. IH NMR (500 MHz, DMSO) delta 10.19 (s, IH), 8.18(d, 2H, J=7.1Hz), 8.16 (s, IH), 7.92 (d, 2H, J=9Hz),7.71 (s, IH), 7.5(d, 2H, J=9Hz), 7.09 (d, 2H, J=8.7Hz), 3.37 (m, 4H), 3.28 (s, 2H), 2.69 (m, 4H), 2.57 (s, 3H). LC/MS: 530 (M+l); HPLC A 3.38 min., 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK & CO., INC.; WO2007/70173; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

75336-86-6, Step 1: 3-(R)-Methyl-piperazine-1-carboxylic Acid Tert-Butyl Ester Triethylamine (3 g, 4.2 mL, 30 mmol) was added to a solution of (R)-2-methyl piperazine (2 g, 20 mmol) in dichloromethane (40 mL) followed by di-tert-butyl-dicarbonate (4.8 g, 22 mmol). The reaction mixture was stirred at room temperature for 20 h. The mixture was diluted with dichloromethane and washed with saturated aqueous sodium bicarbonate and brine and dried over sodium sulfate. The crude product was purified using a short plug of silica gel using hexane/ethyl acetate (1:1). 1H-NMR (CDCl3) delta: 1.05 (3H, d), 1.45 (9H, s), 2.11 (1H, s), 2.37-2.44 (1H, m), 2.66-2.79 (3H, m), 2.93-2.96 (1H, m), 3.93 (2H, br s). ESI-MS m/z: 201(M+1).

As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference£º
Patent; Luly, Jay R.; Nakasato, Yoshisuke; Ohshima, Etsuo; Harriman, Geraldine C.B.; Carson, Kenneth G.; Ghosh, Shomir; Elder, Amy M.; Mattia, Karen M.; US2005/70549; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 145 Synthesis of 2-(4-{6-[7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-ylamino]-2-methyl-pyrimidin-4-yl}-piperazin-1-yl)-ethanol To synthesize the title compound (CLXIX), two intermediate compounds 62 (2-[4-(6-chloro-2-methyl-pyrimidin-4-yl)-piperazin-1-yl]-ethanol) and 63 (7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-ylamine) shown below were used. To synthesize compound 62, to a solution of 4,6-dichloro-2-methyl-pyrimidine (5.0 g, 31 mmol) and 2-piperazin-1-yl-ethanol (2.7 g, 21 mmol) in dioxane (25 mL) was added DIPEA (3.0 mL, 17 mmol). The mixture was heated at reflux for 16 h. The mixture was allowed to cool to room temperature and poured into water. The reaulting aqueous layer was extracted with EtOAc and the combined organic layers washed with brine, dried over Na2SO4 and filtered. The filtrate was concentrated and the residue purified by flash chromatography on silica gel (5-10% MeOH/DCM) to afford compound 62 as a brown liquid (2.1 g, 39%). MS (ESI+): m/z 257.

103-76-4, 103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TargeGen, Inc.; US2005/245524; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics