Downstream synthetic route of Piperazin-2-one

5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5625-67-2, To a stirred solution of piperazin-2-one CK (3 g, 30 inmol) in CHjCfe (50 mL) under argon atmosphere were added tiiethylamine (8.65 mL. 60 mmol) and di-t-buryi dicarbonate (Boc anhydride, 8.2 mL, 36 niniol) at 0 C. The reaction was wanned to RT and stirred for 16 h. The reaction was diluted with water (100 mL) and the product was extracted with CC (2 x 100 mL). The combined organic layers were dried over anhydrous Na S< and concentrated under reduced pressure to obtain Compound CO (4 g, 20 mmol, 66 %) as a white solid, which was used in the next step without further purification. H NMR (400 MHz, CDCi3): delta 6.90 (br s. IH), 4.08 (s, 2H), 3.63-3.59 (m, 2H), 3.35-3.31 (m, 2H), 1.44 (s. 9H). 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields. Reference£º
Patent; VIAMET PHARMACEUTICALS, INC.; YATES, Christopher, M.; SHAVER, Sammy, R.; HOEKSTRA, William, J.; (455 pag.)WO2017/117393; (2017); A1;,
Piperazine – Wikipedia
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Analyzing the synthesis route of Piperazin-2-one

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

5625-67-2,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.

To a stirred solution of W-l (20.0 g, 0.200 mol) in DCM, is added Boc anhydride (43.6 g, 0.200 mol), and TEA (40.4 g, 0.400 mol). The mixture is stirred at about 25 C for about 18 hours. The mixture is concentrated and the residue dissolved in EtOAc then extracted with water. The organic layer is concentrated and the residue is purified by silica gel chromatography to give W-2.

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

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BRUNETTE, Steven, Richard; ABEYWARDANE, Asitha; BURKE, Michael, J.; KAPADIA, Suresh, R.; KIRRANE, Thomas, Martin, Jr.; NETHERTON, Matthew, Russell; RAZAVI, Hossein; RODRIGUEZ, Sonia; SAHA, Anjan; SIBLEY, Robert; SMITH KEENAN, Lana, Louise; TAKAHASHI, Hidenori; TURNER, Michael, Robert; WU, Jiang-Ping; YOUNG, Erick, Richard, Roush; ZHANG, Qiang; ZHANG, Qing; ZINDELL, Renee, M.; WO2013/134226; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 5625-67-2

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

5625-67-2,5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Triethylamine (3.83 mL) and di-tert-butoxydicarbonate (6.32 mL) were added to a mixed solution of piperazin-2-one (2.5 g) in tetrahydrofuran (50 mL) and methanol (50 mL) at room temperature, and the resultant mixture was stirred for 4 hours. The reaction solvent was evaporated under reduced pressure, water and ethyl acetate were added to the residue thus obtained, and the mixture was partitioned. The organic layer was washed with water and saturated saline in this order, and then the washing water layer was combined for further extraction with ethyl acetate. The organic layers were combined and dried over anhydrous magnesium sulfate. After separation by filtration, a residue obtained by evaporating the solvent under reduced pressure was solidified using ethyl acetate-hexane, thus to obtain 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).1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester To a mixed solution of piperazin-2-one (5.07 g) in tetrahydrofuran (50 mL) and methanol (50 mL), triethylamine (7.76 mL) and di-tert-butyl dicarbonate ester (12.17 g) were added at room temperature, and the resultant mixture was stirred for 4 hours. The solvent of the reaction solution was evaporated under reduced pressure, diethyl ether was added to a residue thus obtained, and the precipitated solid was filtered, to obtain 3-oxopiperazine-1-carboxylic acid tert-butyl ester (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-MSm/z: 201(M+H)+.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1785418; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 5625-67-2

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

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.

A) 3-Oxo-piperazine-l-carboxylic acid tert-butyl ester: Piperazinone (20 g, 0.20 mol) was dissolved in 120 mL iV,iV-dimethylformamide. Di-tert- butyldicarbonate (47.9g, 0.20 mmol) was added in portions. After 5 minutes the product precipitated. The solids formed were filtered and dried and used further in step B.1HNMR (400 MHz, chloroform-das solvent and internal reference) delta(ppm) 1.46 (s, 9H), 3.37 (m, 2H), 3.62 (t, 2H, J = 5.1 Hz), 4.08 (s, 2H)., 5625-67-2

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2007/8144; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 5625-67-2

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

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.

Reference Example 50: 3 -Oxo-4-(2-trimethylsilanyl-ethoxymethyl)-piperazine-l -carboxylic acid benzyl ester.; Piperazin-2-one (2.00 g, 20.0 mmol) was dissolved in H2O (10 ml) – 1,4-dioxane (10 ml); and NaHCO3 (1.85 g, 22.0 mmol) and benzylchloroformate (3.42 g, 20.0 mmol) was added thereto. After stirring at room temperature for 13 h, the reaction mixture was diluted with H2O and EtOAc. The aqueous layer was extracted with EtOAc and the combined organic layer was washed with brine, dried over MgSOphi The desiccant was removed through filtration and the filtrate was concentrated under reduced pressure to obtain crude 3 -Oxo-piperazine-1 -carboxylic acid benzyl ester as pale brown oil. This oil was used for the next step without further purification. The crude 3 -Oxo-piperazine-1 -carboxylic acid benzyl ester was dissolved in DMF (40 ml) and NaH (55% in oil, 1.05 g, 24.0 mmol) and SEMCl (5.01 g, 30.0 mmol) was added thereto at room temperature. After stirring at 500C for 18 h, the reaction mixture was diluted with EtOAc. The mixture was washed with H2O and brine, dried over MgSOphi The desiccant was removed through filtration and the filtrate was concentrated under reduced pressure. The EPO residue was purified by silica gel column chromatography (hexane / EtOAc = 8 / 2 to 5 / 5, to obtain the intended compound as a colorless oil.

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK & CO., INC.; BANYU PHARMACEUTICAL CO., LTD.; WO2007/11809; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 5625-67-2

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

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5625-67-2, Piperazine -2-one( 2g, 20 mmol) is added to DCM (30 mL) ,and under the protection of argon Et3N (3.46 mL, 24 mmol) is added ,after cooling down the room temperature to 0 , add BOC anhydride (4.79g, 22mmol) in one reaction flask and raise the room temperature . After 3 h, reaction is stopped and DCM (100 mL) is added, washed with saturated NaCl solution (30 mL x 2), dried over anhydrous magnesium sulfate, concentrated, and recrystallized from DCM and petroleum ether to give a white solid 2.8 g, yield 70%.

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

Reference£º
Patent; Chinese Academy Of Medical Sciences Pharmaceutical Institute; Xu Boling; Chen Xiaoguang; Zhou Jie; Ji Ming; Yao Haiping; Zhou Qin; (57 pag.)CN107098886; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics