Month: June 2021

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

Benzyl 4-(2-hydroxyethyl)piperazine-l-carboxylate (SD038) Benzylchloroformate (4.7 g, 27.6 mmol) in acetonitrile (30 mL) was added dropewise over 30 min to a solution of 1 -(2-hydroxyethyl)piperazine (3 g, 23 mmol) in water (30 mL) via an isobar cylindrical funnel. The pH was maintained around 8-9 by addition of a solution of NaOH 4N. The reaction was stirred overnight at room temperature. The mixture was first extracted with dichloromethane (100 mL) in order to remove the diprotected compound and then acidified with HC1 4N. The acidic aqueous phase was extracted twice with dichloromethane (2 x 100 mL). The organic phase was washed with brine and dried over anhydrous Na2S04. The solvent was removed under vacuum and the crude was purified by flash chromatography with the gradient of methanol in dichloromethane (0-8%) to yield 5.41 g (90%) of product SD038 as a colorless oil.

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; PRESIDENT AND FELLOWS OF HARVARD COLLEGE; HALPERIN, Jose A.; CHOREV, Michael; AKTAS, Bertal Huseyin; WO2014/47437; (2014); 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.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.,55121-99-8

Step 3: l-(4-Bromo-phenyl)-3-[4-(4-methyl-piperazine-l-carbonyl)-phenyl]-urea rTo a solution of (4-amino-phenyl)-(4-methyl-piperazine-l-yl)-methanone (10.0 g, 0.0456 mol) and TEA (4.7 g, 0.0456 mol) in DCM (150 mL) was added 4-bromophenyl isocyanate (10.9 g, 0.0547 mol). The reaction mixture was stirred at room temperature for 12 h. The white solid was obtained and was filtered and dried to afford the title compound [15.0 g, 79%]; LC-MS (ESI): Calculated mass: 416.1; Observed mass: 417.1 [M+H]+ (RT: 0.23 min).

As the paragraph descriping shows that 55121-99-8 is playing an increasingly important role.

Reference：
Patent; ENDO PHARMACEUTICALS INC.; SMITH, Roger, Astbury; THOMPSON, Scott, Kevin; HOSAHALLI, Subramanya; BEJUGAM, Mallesham; NANDURI, Srinivas; PANIGRAHI, Sunil, Kumar; MAHALINGAM, Natarajan; WO2012/58671; (2012); 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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 4-chloro-3-methyl-5-phenyl-1,1-pyrazolo[3,4-c]pyridazine (0.33 mmol), the alcohol (0.65 mmol), diethyl azodicarboxylate (114 mg, 0.65 mmol) and triphenyl phosphine (171 mg, 0.65 mmol) in 1,4-dioxane (2 mL) was heated using microwave irradiation to a temperature between 85 and 120° C. for a 30 to 90 min period. The reaction mixture was concentrated in vacuo and the residue was purified by preparative HPLC to provide the title compound.4-chloro-3-methyl-1-[2-(4-methylpiperazin-1-yl)ethyl]-5-phenyl-pyrazolo[3,4-c]pyridazine (Compound Iv) Compound Iv was synthesized from 4-chloro-3-methyl-5-phenyl-1H-pyrazolo[3,4-c]pyridazine and 2-(4-methylpiperazin-1-yl)ethanol following the general procedure for the Mitsunobu reaction described above. 1H NMR delta (ppm) (CHCl3-d): 7.80-7.77 (2H, m), 7.56-7.48 (3H, m), 4.80 (2 t), 2.99 (2H, t), 2.80 (3H, s), 2.64 (4H, br s), 2.40 (4H, br s), 2.26 (3H, s). LCMS (10 cm_ESCI_Formic_MeCN) Rt 2.53 min; m/z 371 [M+H] 99.25percent purity., 5464-12-0

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

Reference：
Patent; BUeRLI, Roland Werner; ESMIEU, William Rameshchandra Krishna; LOCK, Christopher James; MALAGU, Karine Fabienne; OWENS, Andrew Pate; HARTE, William E.; US2014/121197; (2014); 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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

A mixture of 7-(6-Chloro-pyrimidin-4-yloxy)-isoquinoline-4-carboxylic acid (1.95 g, 5.5 mmol), 4-(4- Methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (1.5 g, 5.49 mmol) and triethylamine (6.42 mL, 46.2 mMol) in dry DMF (50 mL) is heated under an argon atmosphere at 500C. A solution of propylphosphonic anhydride (5.4 mL, 8.2 mmol) 50% inDMF is then added. After 2 h, the reaction mixture is poured onto an aqueous solution of NaHCO3 and stirred at 00C for 1h. The suspension is then filtered (hyflo) and the solid residue is dissolved in CH2CI2 – MeOH (5:1). The solvent is evaporated off under reduced pressure to afford a crude product which is purified by reversed phase MPLC (Bchi system), yielding, after neutralisation with saturated aqueous NaHCO3, the title compound as a orange solid., 694499-26-8

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2007/31265; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

10A. (E)-3-(4-Fluorophenyl)-1-(4-isopropylpiperazin-1-yl)prop-2-en-1-one To a solution of E-4-fluorocinnamic acid (1.18 g, 7. 10 mmol), which is commercially available from Sigma-Aldrich, and TBTU (3.42 g, 10.6 mmol) in DMF (50 mL) was added 1-isopropylpiperazine (1.12 mL, 7.81 mmol) at ambient temperature. The reaction was stirred for ca. 15.5 h before being concentrated under reduced pressure, wherein the crude residue was dissolved in EtOAc (70 mL) and partitioned with sat. aq. NaHCO3 (25 mL). The aq. layer was separated and further extracted with EtOAc (2.x.30 mL). The combined organic layers were then washed with sat. aq. NaHCO3 (2.x.20 mL) and brine (35 mL), then concentrated in vacuo. The resulting residue was subjected to flash chromatography (SiO2-40 g; gradient elution: 100percent DCM for 5 min, then 0percent to 2percent MeOH/DCM over 5 min; hold for 5 min, 2percent to 4percent over 5 min, hold for 5 min, 4percent to 10percent over 5 min, hold 10percent MeOH/DCM for 5 min at 40 mL/min) to give 1.58 g 10A (80percent yield) as a pale orange solid. m/z (ES+) M+1=277.4; HPLC tR=1.50 min. 1H NMR (500 MHz, CDCl3) delta 7.62 (d, J=15.6 Hz, 1H), 7.50 (dd, J=8.9, 5.5 Hz, 2H), 7.11-6.99 (m, 2H), 6.80 (d, J=15.6 Hz, 1H), 3.85-3.54 (m, 4H), 2.73 (quintet, J=6.7 Hz, 1H), 2.55 (d, J=5.2 Hz, 4H), 1.05 (d, J=6.4 Hz, 6H).

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; US2009/76020; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 98 1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-[4-(2-oxo-1-piperazinyl)phenyl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one To 6-(4-iodophenyl)-1-(4-methoxyphenyl)-3-(methylsulfonyl)-1,4,5,6-tetrahydro-7H-pyrazolo(3,4-c)pyridin-7-one (0.55 g, 1.0 mmol), 4-benzyloxycarbonylpiperazin-2-one (0.35 g,1.4 mmol),and K2CO3 (0.23 g,1.6 mmol) was added DMSO (5 mL). The mixture was degassed with N2. CuI (39 mg, 0.21 mmol) was added and the reaction was heated to 130 C. for 18 h. The reaction was diluted with EtOAc and water, extracted with EtOAc, and dried (MgSO4). Purification of the intermediate by chromatography on silica gel using 5%MeOH/CH2Cl2 was followed by deprotection in refluxing TFA. Purification by HPLC and freeze-drying afforded 175 mg (27%) of a white solid; High Resolution Mass Spec (M+H)+for C24H26N6O5S 496.1650.

78818-15-2, As the paragraph descriping shows that 78818-15-2 is playing an increasingly important role.

Reference：
Patent; Pinto, Donald J.P.; Quan, Mimi L.; Orwat, Michael J.; Li, Yun-Long; Han, Wei; Qiao, Jennifer X.; Lam, Patrick Y.S.; Koch, Stephanie L.; US2003/191115; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution OF RAC-3-METHYL-PIPERAZINE-L-CARBOXYLIC acid tert-butyl ester (350 mg, 1.75 mmol) in dimethylformamide (3 ml) were added 2-Iodo-5-methanesulfonyl-benzoic acid (540 mg, 1.67 mmol), N-ETHYLDIISOPROPYLAMINE (1. 8 ml, 10.5 mmol), and TBTU (630 mg, 1.92 mmol). The reaction mixture was then allowed to stir at room temperature for 16 hours. The reaction mixture was then concentrated in vacuo and the residue was purified by column chromatography (SI02, 20g, Heptane/EtOAc 0-100percent) to give the title compound (400 mg, 45 percent). MS (m/e): 526.2 (M+NH4+).

120737-59-9, As the paragraph descriping shows that 120737-59-9 is playing an increasingly important role.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; WO2005/23260; (2005); 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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

A mixture of 1 ,1-dimethylethyl 3-oxo-1-piperazinecarboxylate (0.200 g, 0.999 mmol), 1-bromo-4-fluorobenzene (0.091 mL, 0.832 mmol), copper(l) iodide (0.008 g, 0.042 mmol), potassium carbonate (0.230 g, 1.665 mmol) and N,N’-dimethyl-1 ,2- ethanediamine (0.009 mL, 0.083 mmol) in toluene (5 mL) was heated at reflux under nitrogen overnight. The reaction mixture was filtered through silica gel. The filtrate was evaporated and the residue was purified by silica gel chromatography (EtOAc:hexane) to give1 ,1-dimethylethyl 4-(4-fluorophenyl)-3-oxo-1-piperazinecarboxylate (0.180 g, 73%) as a white solid., 76003-29-7

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; PEAT, Andrew, James; PRICE, Daniel, J.; SHOTWELL, John, Brad; TAI, Vincent; ZHANG, Huichang; WO2011/41713; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,6-difluoro-3-(oxiran-2-yl)benzonitrile (1.50 g, 8.28 mmol) and (S)-4-N-BOC-2-hydroxymethylpiperazine (2.40g, 11.1 mmol) were suspended in ethanol (15 mL) then heated in a microwave apparatus for 30 min at 150 C. Thereaction mixture was cooled and evaporated dryness. The residue was purified by chromatography through a 120gRedi-sep column eluting with 5%MeOH/95% EtOAc to yield the title compound LC-MS: M+1 = 398

314741-40-7, The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Merck Sharp & Dohme Corp.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Example 62A tert-butyl (2R)-2-methyl-4-[(6-{[6-(trifluoromethyl)pyridin-3-yl]oxy}quinolin-2-yl)carbonyl]piperazine-1-carboxylate The titled compound was prepared using the reaction conditions described for Example 1E, substituting 6-{[6-(trifluoromethyl)pyridin-3-yl]oxy}quinoline-2-carboxylic acid for 6-{[5-(trifluoromethyl)pyridin-2-yl]oxy}quinoline-2-carboxylic acid and (R)-tert-butyl 2-methylpiperazine-1-carboxylate for tert-butyl piperazine-1-carboxylate (254 mg, 82%).

120737-78-2, As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference：
Patent; AbbVie Inc.; Bogdan, Andrew; Cowart, Marlon D.; DeGoey, David A.; Jinkerson, Tammie K.; Koenig, John R.; Kort, Michael E.; Liu, Bo; Matulenko, Mark A.; Nelson, Derek W.; Patel, Meena V.; Peltier, Hillary; Scanio, Marc J.; Wakefield, Brian D.; US2015/218102; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics