Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

Example 21 7-[(4-tert-Butoxycarbonylpiperazin)-1-yl]-1-ethyl-8-methoxy-2,3,4,5-tetrahydro-1H-1-benzazepine-2-one An oven-dried flask, charged with 7-bromo-1-ethyl-8-methoxy-2,3,4,5-tetrahydro-1H-1-benzazepine-2-one (268 mg, 0.90 mmol), benzyl 1-piperazinecarboxylate (201 mg, 1.08 mmol), Pd(OAc)2 (20.16 mg, 0.09 mmol, 10 mol percent), BINAP (84.12 mg, 0.134 mmol) was purged with argon for 5 min. Anhydrous toluene (1.5 mL) was added via syringe. The flask was opened and sodium tert-butoxide (120.0 mg, 1.26 mmol) was added in one portion. After purging with argon for 3 min, the reaction mixture was stirred and heated at 100¡ã C. for 2 hrs. TLC indicated that the starting material has been consumed. The reaction mixture was allowed to cool to ambient temperature, poured into water, extracted with ethyl acetate, dried over Na2SO4, filtered and evaporated to dryness. Purification of the crude product by flash chromatography on silica gel column eluted with MeOH/DCM (10percent of MeOH in DCM) gave the title compound as brownish foam (266 mg, 73percent). M.P.: amorphous compound MS (FAB): calcd for C22H33N3O4 403.52; found m/e 404 (M+1)+., 31166-44-6

The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Antex Pharma Inc.; US6514965; (2003); B1;,
Piperazine – Wikipedia
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142-64-3, Piperazine Dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,142-64-3

EXAMPLE 27 In a 100-ml. flask was placed 1.59 g. of piperazine dihydrochloride and 3 ml. of water. To the resulting solution was added 3.92 g. of 2,3,4-trimethoxybenzaldehyde dissolved in 15 ml. of methanol. A solution of 0.98 g. of sodium cyanide in 5 ml. of water was added dropwise to the mixture over a period of about 10 minutes with ice cooling. Then the reaction mixture, from which crystalline precipitate separated upon heating, was stirred for 2.5 hours while the external temperature was kept at 40 to 50C. After the mixture was cooled, crystal was collected by filtration, washed with water and methanol, and dried. There was obtained 4.3 g. of crystal having a melting point of 244 – 247C. Recrystallization from chloroform-methanol afforded N,N’-bis-(alpha-cyano-2,3,4-trimethoxybenzyl)piperazine as a crystalline product melting at 245 – 247C.

The synthetic route of 142-64-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Fuji Chemical Industry Co., Ltd.; Nippon Chemiphar Co., Ltd.; US3962247; (1976); A;,
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.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A solution of 2-chloroalkyl/aryl substitutedwith or without N-substitution as well as with or without 5 and/or 6-substituted benzimidazole derivative (1.75g,0.01051mol) and 1-[(4-phenyl)carbonyl]piperazine (3g,0.0105mol) in N, N dimethylformamide was taken in a RBF.K2CO3(2gm,) was added to the reaction mixture. The reaction mixture was stirred for 8h at 80C on a magnetic stirrer (heat + stirring). The progress of the reaction was monitored by thin layer chromatography (TLC).Upon completion of the reaction, water was added to the reaction mixture and the product extracted by shaking the reaction mixture with dichloromethane in a separating funnel.The dichloromethane layer was washed successively with water and brine, dried over anhydrous sodium sulfate. Evaporation of the solvent gave theproduct. 11a-l Recrystallized with various solvent like chloroform, ethanol, methanol., 13754-38-6

As the paragraph descriping shows that 13754-38-6 is playing an increasingly important role.

Reference£º
Article; Kankate, Rani S.; Gide, Parag S.; Belsare, Deepak P.; Oriental Journal of Chemistry; vol. 30; 4; (2014); p. 1855 – 1863;,
Piperazine – Wikipedia
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

Example 46; 8-Ethyl-2- { [4-(4-ethylpiperazin- 1 -yl)phenyl] amino } -4-methyl-6-phenylpyrido [2,3 – d]pyrimidm-7(8H)-one[00242] 8-Ethyl-4-methyl-2-(methylsulfonyl)-6-phenylpyrido[2,3-cdpyrimidin-7(8H)- one (275 mg, 0.80 mmol) and 4-(4-ethylpiperazin-l-yl)aniline (197 mg, 1.2 equiv.) were added to dimethyl sulfoxide (5 mL) and the resulting mixture was heated to 100 0C and stirred overnight. After cooling to room temperature, the reaction was partitioned between aqueous and organic layers with ethyl acetate and H2O, organic layer was dried with anhydrous magnesium sulfate, filtered and evaporated, and directly applied to prep-LC to EPO provide the title compound in (210.0 mg, 56 % yield): 1H NMR (400 MHz, CDCl3): delta 7.80(s, IH), 7.62 (d, 2H), 7.60 (d, 2H)5 7.40 (m, 2H), 7.18 (s, 1eta), 6.95 (d, 2H)5 4.50 (q, 2H)5 3.22(m, 4H)5 2.70 (m, 4H)5 2.60 (s, 3H)5 2.50 (m, 2H)5 1.40 (t, 3H)5 1.20 (t, 3H); MS (EI) forC28^2N6O: 469.10 (MH4)., 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.; WO2007/44698; (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.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 6-(tert-butylsulfonyl)-4-((5-fluoro-lH-indazol-3-yl)amino)quinolin-7-ol (100 mg, 0.24 mmol) and tert-butyl 4-(2-chloroethyl)piperazine-l-carboxylate (72 mg, 0.20 mmol) in N,N- Dimethylformamide (DMF) (0.8 mL) was added potassium carbonate (50.0 mg, 0.36 mmol) and sodium iodide (7.2 mg, 0.05 mmol). The reaction was warmed to 50 C and stirred under an atmosphere of nitrogen. It was cooled to room temperature and concentrated under vacuum. The residue was subjected directly to purification by flash chromatography (60g pre-packed C-18 SNAP cartridge: 40% to 90% acetonitrile (0.1% ammonia) in water (10 mM ammonium bicarbonate)). The desired fractions were combined and concentrated to afford the title compound (100 mg, 0.16 mmol, 66 % yield). LCMS Method B T= 1.18 min, ES+ve 627.

208167-83-3, As the paragraph descriping shows that 208167-83-3 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; CASILLAS, Linda N.; HARLING, John David; MIAH, Afjal Hussain; SMITH, Ian Edward David; RACKHAM, Mark David; (204 pag.)WO2017/182418; (2017); A1;,
Piperazine – Wikipedia
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109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

PREPARATION 2 2-(4-methylpiperazin-1-yl)-aniline A mixture of 2-fluoronitrobenzene (6.0 mL, 56.9 mmol) and N-methylpiperazine (8.11 mL, 56.9 mmol) was stirred at 0 C. for 20 minutes, then at room temperature for 3 days. The crude mixture was partitioned between methylene chloride and saturated aqueous sodium bicarbonate and the organic layer was then washed with saturated sodium chloride (NaCl), dried and concentrated in vacuo to provide 2-(4-methylpiperazin-1-yl)-1-nitrobenzene as an orange oil, 12.4 g. 1H-NMR (CDCl3, 300 MHz) delta 7.75 (1H, dd), 7.47 (1 H, dt) 7.15 (1H, dd), 7.03 (1H, dt), 3.09 (1H, dd), 2.56 (1H, dd), 2.36 (3H, s).

109-01-3, 109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Pfizer Inc.; US6258953; (2001); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

304897-49-2, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Commercially available benzoic acid (1.3 mmol) was suspended in toluene (0.01 M), thionyl chloride (12 mmol) was added and the mixture was heated at 110 00for lh. Volatiles were evaporated and the residue was added to a solution of the intermediate of formula (X) (compounds of examples 4-6 of Table 2)(1 mmol) in pyridine (40 mmol) and the resulting mixture stirred for 1 h at rt. Pyridine was evaporated, then NaOMe (2 mmol) and MeOH were added. After 30 minutes solvent was evaporated and DCM and water were added. The separated organic phase was concentrated and the residue was purified by flash chromatography eluting with DCM/MeOH to give the compounds of examples 11,12,13.

304897-49-2, The synthetic route of 304897-49-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ROTTAPHARM BIOTECH S.R.L.; ARTUSI, Roberto; CASELLI, Gianfranco; ROVATI, Lucio; (78 pag.)WO2016/146220; (2016); 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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

For the N-boc protection of amines, to solution of diboc (1 mmol) in ethanol (5 ml) was added {K*18-crown-6]Br3}n (0.001 mmol). The solution was stirred at room temperature for 1 min. The amine (1 mmol) was then added and solution as stirred at room temperature for an appropriate time (table 1). After completion of the reaction, the solvent was removed by water bath distillation. To the residue was added ethyl acetate (5 ml) and the mixture was filtered (the catalyst is insoluble in n-hexane and ethyl acetate). The solid was washed with ethyl acetate ()10 ml*2) amd combined filtrates were reduced to dryness to yield the pure products.

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

Reference£º
Article; Chehardoli, Gholamabbas; Zolfigol, Mohammad Ali; Derakhshanpanah, Fateme; Cuihua Xuebao/Chinese Journal of Catalysis; vol. 34; 9; (2013); p. 1730 – 1733;,
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.132710-90-8,1-Boc-4-(3-hydroxypropyl)piperazine,as a common compound, the synthetic route is as follows.,132710-90-8

A mixture of tert-butyl 4-(3-hydroxypropyl)piperazine-l-carboxylate (1.52 g, 6.2 mmol), Ph3P (2.46 g, 9.4 mmol), I2 (2.40 g, 9.4 mmol) and imidazole (1.28 g, 18.6 mmol) in DCM (100 mL) was stirred at room temperature for 5 h. The mixture was diluted with DCM and the organic layer was washed with brine, dried over anhydrous sodium sulfate, filtered, and evaporated under vacuum to give a residue which was purified by column chromatography (silica gel, PE : EtOAc = 5 : 1) to afford tert-butyl 4-(3-iodopropyl)piperazine-l-carboxylate (1.10 g, 50% ) as a colorless oil.

The synthetic route of 132710-90-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PRINCIPIA BIOPHARMA INC.; BRAMELD, Kenneth Albert; VERNER, Erik; (122 pag.)WO2016/191172; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N-(ira^-4-(3-Chloropyrazin-2-yloxy)cyclohexyl)benzo[JJthiazol-2-amine (0.080 g, 0.22 mmol), 1 -methylpiperazin-2-one hydrochloride (0.10 g, 0.67 mmol), and triethylamine (0.093 mL, 0.67 mmol) were mixed in DMSO (2 mL) under an argon atmosphere. The reaction mixture was stirred at 80 C for 24 h. The reaction mixture was then warmed to 120 C and stirred for an additional 72 h. The reaction mixture was cooled to T, diluted with water, and extracted with EtOAc (2x). The organic extracts were combined, washed with saturated sodium chloride, dried over magnesium sulfate, filtered, and concentrated. The resulting crude product was purified via silica gel chromatography to give 4-(3-(ira?s-4-(benzo[J]thiazol-2- ylamino)cyclohexyloxy)pyrazin-2-yl)-l-methylpiperazin-2-one as a light orange solid. [M+l] 439.2. ICso (uM): 0.5369., 109384-27-2

109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AMGEN INC.; ALLEN, Jennifer; FROHN, Michael; HARRINGTON, Paul; PICKRELL, Alexander; RZASA, Robert; SHAM, Kelvin; HU, Essa; WO2011/143366; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics