Category: 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,5625-67-2

A 2-L Erlenmeyer flask was charged with 2-piperazinone (36.5 g, 364 mmol, Sigma- Aldrich, St. Louis, MO), sodium carbonate (116 g, 1093 mmol), 600 mL of dioxane, and 150 mL of water. To this was slowly added benzyl chloroformate (62.1 g, 364 mmol, Sigma-Aldrich, St. Louis, MO) at room temperature over 20 min. After the addition was complete, the mixture was stirred for 2 h and then diluted with water and extracted with EtOAc (2 L). The combined organic extracts were dried (MgS04), filtered, and concentrated to give a white solid. To this solid was added 500 mL of DCM, triethylamine (128 mL, 911 mmol), DMAP (4.45 g, 36.4 mmol), and di-tert-butyl dicarbonate (119 g, 546 mmol, Sigma-Aldrich, St. Louis, MO). After 1 h at room temperature, the mixture was diluted with water and the organics were separated. The organics were dried (MgS04), filtered, and concentrated to give a brown oil. To this oil was added 100 mL of DCM followed by 1 L of hexane. The resulting white solid was collected by filtration to give 4-benzyl 1-tert-butyl 2-oxo-l,4- piperazinedicarboxylate (101 g).

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

Reference：
Patent; AMGEN INC.; ASHTON, Kate; BOURBEAU, Matthew, Paul; HONG, Fang-Tsao; LIU, Longbin; NISHIMURA, Nobuko; NORMAN, Mark, H.; POON, Steve, F.; STEC, Markian, M.; ST. JEAN, David, J., JR; TAMAYO, Nuria, A.; YANG, Kevin, C.; WO2013/123444; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

EXAMPLE 2 t-Butyl 3-Oxo-1-piperazinecarboxylate (2) To a mixture of piperazinone 1 (1.0 g, 1.0*10-2 mole) and sieve dried THF (15 ml) is added dropwise a solution of di-tert-butyl dicarbonate (2.4 g, 1.1*10-2 mole) and sieve dried THF (5 ml). Evolution of CO2 occurs immediately and the starting material slowly dissolves. After stirring at room temperature overnight the solvent is evaporated at reduced pressure affording 2 as a beige solid which crystallized from ethyl acetate/hexane as colorless plates: 1.2 g (60%), m.p. 159-161 C.

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

Reference：
Patent; Richardson-Merrell Inc.; US4341698; (1982); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

2-Piperazinone (2.5 g; 24.97 mmol) was dissolved in DCM ( 55 ml ). A solution of tert- butyloxycarbonyl anhydride (5.45g, 24.97mmol) in DCM (20 ml) was added dropwise. The reaction mixture was stirred at room temperature for 4 h. The reaction mixture was concentrated to dryness and dried under high vacuum, at room temperature. The residue containing Int. 177 (5.1 g) was used as such in the next reaction step.

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

Reference：
Patent; JANSSEN PHARMACEUTICA NV; DIELS, Gaston, Stanislas, Marcella; SCHOENTJES, Bruno; VERSELE, Matthias, Luc, Aime; BERTHELOT, Didier, Jean-Claude; WILLEMS, Marc; VIELLEVOYE, Marcel; EMBRECHTS, Werner, Constant, Johan; WROBLOWSKI, Berthold; MEERPOEL, Lieven; WO2015/150555; (2015); 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, Piperazin-2-one (10 g, 0.1 mol), Et3N (20.2g, 0.2 mmol) and DCM (100 mL) were combined and cooled to 0 C. To the solution was added Boc20 (26.1 g, 0.12 mol) in DCM (250 ml), and the resulting mixture was warmed to room temperature and stirred for 12 h. The reaction mixture was concentrated and dissolved in ethyl acetate, washed with 1 N HC1, brine, dried over sodium sulfate, filtered and concentrated. The crude product was used without further purification. (19.5 g, yield 97.5%).

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

Reference：
Patent; EPIZYME, INC.; DUNCAN, Kenneth, W.; CHESWORTH, Richard; MUNCHHOF, Michael, John; WO2014/100716; (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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, Di-tert-butyl dicarbonate (3.92 g, 17.98 mmol) was added to a suspension of 2-piperazinone (1.50 g, 14.98 mmol) in dichloromethane (15 mL). The mixture was stirred at room temperature for 5 hours. The solvent was evaporated to afford 1 ,1- dimethylethyl 3-oxo-1-piperazinecarboxylate (2.99 g, quantitative) as an off-white solid.

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

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

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, Di-tert-butyl dicarbonate (3.92 g, 17.98 mmol) was added to a suspension of 2-piperazinone (1.50 g, 14.98 mmol) in dichloromethane (15 mL). The mixture was stirred at room temperature for 5 hours. The solvent was evaporated to afford 1 ,1- dimethylethyl 3-oxo-1-piperazinecarboxylate (2.99 g, quantitative) as an off-white solid.

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

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

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, General procedure: To a solution of 3-aminopyrrolidine-1-carboxylate (744 mg, 4 mmol) in DCM (10 mL) , DIEA(1.04 mL, 6 mmol) and benzyl chloroformate (0.72 mL, 5 mmol) were added at 0. The reactionmixture was stirred at room temperature until TLC monitoring showed that the reaction wascomplete. The mixture was diluted with DCM and washed with water and brine. The organic layerwas dried over anhydrous MgSO4andevaporated, and column chromatography (petroleum ether /ethyl acetate =8:1 to 5:1) to give the corresponding product I-4 as light yellow oil (1.05 g, 82%).

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

Reference：
Article; Zhou, Jie; Ji, Ming; Zhu, Zhixiang; Cao, Ran; Chen, Xiaoguang; Xu, Bailing; European Journal of Medicinal Chemistry; vol. 132; (2017); p. 26 – 41;,
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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

Step 1tert-butyl 4-benzyl-3-oxopiperazine-1-carboxylateDi-tert-butyl dicarbonate (750 mg, 3.44 mmol) was added to a solution of piperazine-2-one (344 mg, 3.44 mmol) in CH2C12 (13 mL). The solution was stirred at room temperature for 16 hours, then concentrated under vacuum. The residue was dissolved in N,Ndimethylformamide (10 mL) and stirred under nitrogen as sodium hydride (60% dispersion in oil, 0.25 g, 6.25 mmol) was added at room temperature. The mixture was stirred for 30 minutes, then benzyl bromide (0.532 mL, 4.47 mmol) was added. The mixture was stirred under nitrogen for 1 hour, and the reaction was quenched by cautious addition of water (3 mL). Finally, the mixture was diluted with water (50 mL) and stirred at room temperature for 2 hours. The resulting precipitate was collected by filtration and washed with water (40 mL), then dried under vacuum to the titled compound (0.82 g, 82%). ?H NMR (400 MHz, methanol-d4) ppm 1.46 (s, 9H), 3.30 – 3.33 (m, 2H), 3.60 (t, J = 5.2 Hz, 2H), 4.11 (s, 2H), 4.62 (s, 2H), 7.25 – 7.37 (m, 5H); MS (ESI) m/z 291 (M+H)., 5625-67-2

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

Reference：
Patent; ABBVIE INC.; SCANIO, Marc; BUNNELLE, William; KOENIG, John Robert; DRIZIN, Irene; PLIUSHCHEV, Marina; COWART, Marlon; WO2015/112445; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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, General procedure: To a solution of 3-aminopyrrolidine-1-carboxylate (744 mg, 4 mmol) in DCM (10 mL) , DIEA(1.04 mL, 6 mmol) and benzyl chloroformate (0.72 mL, 5 mmol) were added at 0. The reactionmixture was stirred at room temperature until TLC monitoring showed that the reaction wascomplete. The mixture was diluted with DCM and washed with water and brine. The organic layerwas dried over anhydrous MgSO4andevaporated, and column chromatography (petroleum ether /ethyl acetate =8:1 to 5:1) to give the corresponding product I-4 as light yellow oil (1.05 g, 82%).

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

Reference：
Article; Zhou, Jie; Ji, Ming; Zhu, Zhixiang; Cao, Ran; Chen, Xiaoguang; Xu, Bailing; European Journal of Medicinal Chemistry; vol. 132; (2017); p. 26 – 41;,
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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

Step 1tert-butyl 4-benzyl-3-oxopiperazine-1-carboxylateDi-tert-butyl dicarbonate (750 mg, 3.44 mmol) was added to a solution of piperazine-2-one (344 mg, 3.44 mmol) in CH2C12 (13 mL). The solution was stirred at room temperature for 16 hours, then concentrated under vacuum. The residue was dissolved in N,Ndimethylformamide (10 mL) and stirred under nitrogen as sodium hydride (60% dispersion in oil, 0.25 g, 6.25 mmol) was added at room temperature. The mixture was stirred for 30 minutes, then benzyl bromide (0.532 mL, 4.47 mmol) was added. The mixture was stirred under nitrogen for 1 hour, and the reaction was quenched by cautious addition of water (3 mL). Finally, the mixture was diluted with water (50 mL) and stirred at room temperature for 2 hours. The resulting precipitate was collected by filtration and washed with water (40 mL), then dried under vacuum to the titled compound (0.82 g, 82%). ?H NMR (400 MHz, methanol-d4) ppm 1.46 (s, 9H), 3.30 – 3.33 (m, 2H), 3.60 (t, J = 5.2 Hz, 2H), 4.11 (s, 2H), 4.62 (s, 2H), 7.25 – 7.37 (m, 5H); MS (ESI) m/z 291 (M+H)., 5625-67-2

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

Reference：
Patent; ABBVIE INC.; SCANIO, Marc; BUNNELLE, William; KOENIG, John Robert; DRIZIN, Irene; PLIUSHCHEV, Marina; COWART, Marlon; WO2015/112445; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics