Category: 76003-29-7

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.

Step 1: ferf-Butyl 3-oxo-4-(3-thienyl)piperazine-l-carboxylate (Hl)A mixture of l-Boc-3-oxopiperazine (1.0 eq.), 3-bromothiophene (1.5 eq.), K3PO4 (2.0 eq.), CuI (0.4 eq.) and lambda^-dimethylethylendiamine (0.8 eq.) in 1,4-dioxane (0.5M) was put in a sealed vial and stirred at 1100C for 18 hr. Reaction mixture was diluted with EtOAc and filtered through a pad of SolcaFloc 200 FCC. After removal of the solvent, the crude product was purified by flash column chromatography on silica gel using 10- 40% EtO Ac/Petroleum ether as eluent to afford the desired product Hl as pink solid (80% yield). 1H NMR (400 MHz, CDCl3, 300K) delta 7.32-7.28 (3H, m), 4.25 (2H, s), 3.82-3.75 (4H, m), 1.49 (9H, s). MS (ES) CnHi8N2 O3S requires: 282, found: 283 (M+H)+.

76003-29-7, The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.; WO2009/63244; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

76003-29-7, A mixture of 1 ,1 -dimethylethyl 3-oxo-1 -piperazinecarboxylate (0.489 g, 2.44 mmol), 3-bromothiophene (0.332 g, 2.036 mmol), copper(l) iodide (0.019 g, 0.102 mmol), potassium carbonate (0.563 g, 4.07 mmol) and trans-N,N-dimethyl-cyclohexane-1 ,2- diamine (0.029, 0.204 mmol) in 1 ,4-dioxane (5 mL) was heated at reflux under nitrogen for 24 hours. After cooling to room temperature, the reaction mixture was filtered through silica ge. eluting with DCM:EtOAc/1 :1 , The filtrate was concentrated and the residue was purified by silica gel chromatography to afford 1 ,1 -dimethylethyl 3-oxo-4-(3-thienyl)-1 – piperazinecarboxylate (0.305 g, 53%) as a white solid.

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

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.,76003-29-7

NaH (60 % in mineral oil) (0.24 g; 5.99mmol) was added to a solution of Int. 177 (1 g; 4.99 mmol) in DMF (8 ml) and cooled to 0 C under N2-gas atmosphere. The mixture was stirred at this temperature for 10 min. Methyl bromoacetate (0.522 mL; 5.49 mmol) was added. The cooling bath was removed and the reaction stirred overnight. Subsequently, the reaction was quenched with H20 (2 ml ). A saturated NaCl aqueous solution (20 ml) was added and the mixture was extracted with EtOAc (14 ml ). The organic layer was dried over MgS04, filtered and concentrated to dryness. The residue was purified by chromatography over silica gel eluting with a gradient from 100 % DCM to 40 % DCM and 60 % DCM/MeOH 9/1, v/v. The desired fractions were collected and the solvent was evaporated. Yield: 1.14 g of Int. 178 (84 %).

As the paragraph descriping shows that 76003-29-7 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

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 121Exam le 121a ieri-Butyl 4-(6-Nitropyridin-3-yl)-3-oxopiperazine-l-carboxylate 121aA 250-mL single-neck round-bottomed flask equipped with a magnetic stirrer and reflux condenser was charged with 2-nitro-5-bromopyridine (1.00 g, 5.00 mmol), 2-oxo-4- (ieri-butoxycarbonyl)piperazine (1.01 g, 5.00 mmol), cesium carbonate (3.58 g, 11.0 mmol) and 1,4-dioxane (40 mL). After bubbling nitrogen through the result-ing solution for 30 min, Xantphos (246 mg, 0.425 mmol) and tris(dibenzylidene-acetone)dipalladium(0) (230 mg, CGIPHARM60WO0.250 mmol) were added, and the reaction mixture was heated at reflux for 6 h. Water (30 mL) and ethyl acetate (150 mL) were added after the reaction mixture was cooled to room temperature. The resulting mixture was filtered through a bed of Celite 521. The organic layer of the filtrate was separated and the aqueous layer was extracted with ethyl acetate (2 x 50 mL). The combined organic layers were washed with brine (30 mL), dried over sodium sulfate and purified by column chromatography to afford a 96% yield (1.55 g) of 121a as an amber oil: ]H NMR (300 MHz, CDC13) delta 8.67 (d, 1H, J = 2.4 Hz), 8.32 (d, 1H, J = 8.7 Hz), 8.15 (dd, 1H, / = 8.7, 2.4 Hz), 4.33 (s, 1H), 3.89 (m, 4H), 1.48 (s, 9H); MS (ESI+) mJz 323.1 (M+H)., 76003-29-7

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GILEAD CONNECTICUT, INC.; GENENTECH, INC.; CURRIE, Kevin S.; WANG, Xiaojing; YOUNG, Wendy B.; WO2012/31004; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 121Exam le 121a ieri-Butyl 4-(6-Nitropyridin-3-yl)-3-oxopiperazine-l-carboxylate 121aA 250-mL single-neck round-bottomed flask equipped with a magnetic stirrer and reflux condenser was charged with 2-nitro-5-bromopyridine (1.00 g, 5.00 mmol), 2-oxo-4- (ieri-butoxycarbonyl)piperazine (1.01 g, 5.00 mmol), cesium carbonate (3.58 g, 11.0 mmol) and 1,4-dioxane (40 mL). After bubbling nitrogen through the result-ing solution for 30 min, Xantphos (246 mg, 0.425 mmol) and tris(dibenzylidene-acetone)dipalladium(0) (230 mg, CGIPHARM60WO0.250 mmol) were added, and the reaction mixture was heated at reflux for 6 h. Water (30 mL) and ethyl acetate (150 mL) were added after the reaction mixture was cooled to room temperature. The resulting mixture was filtered through a bed of Celite 521. The organic layer of the filtrate was separated and the aqueous layer was extracted with ethyl acetate (2 x 50 mL). The combined organic layers were washed with brine (30 mL), dried over sodium sulfate and purified by column chromatography to afford a 96% yield (1.55 g) of 121a as an amber oil: ]H NMR (300 MHz, CDC13) delta 8.67 (d, 1H, J = 2.4 Hz), 8.32 (d, 1H, J = 8.7 Hz), 8.15 (dd, 1H, / = 8.7, 2.4 Hz), 4.33 (s, 1H), 3.89 (m, 4H), 1.48 (s, 9H); MS (ESI+) mJz 323.1 (M+H)., 76003-29-7

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GILEAD CONNECTICUT, INC.; GENENTECH, INC.; CURRIE, Kevin S.; WANG, Xiaojing; YOUNG, Wendy B.; WO2012/31004; (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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

Step A1, 1-dimethylethyl 4-(2-fIuoro-4-methylphenyl)-3-oxo-1-piporazinecarboxylate A mixture of 1 ,1-dimethylethyl 3-oxo-1 -piperazinecarboxylate (0.326 g, 0.00163 mol), 1-bromo-2-fluoro-4-methylbenzene (0.308 g, 0.0163 mol), (1 R,2R)-N,N’-dimethyl~ 1 ,2-cyclohexanediamine (0.026 mL, 0.163 mmol), copper(l) iodide (3.10 mg, 0.016 mmol) and potassium carbonate (450 mg, 3.26 mmol) in 1 ,4-dioxane (6 mL) in a septum-sealed vial was heated in an oil bath at 120 C overnight. The reaction mixture was cooled to room temperature and filtered through Celite washing with ethyl acetate. The filtrate was washed with saturated aqueous ammonium chloride, water and brine, dried over sodium sulfate and concentrated. The residue was purified by chromatography on silica gel to give the title compound (0. 253 g, 50%). MS (ESI) m/z: 309 (M+1 )., 76003-29-7

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; MAYNARD, Andy; MILLER, John; PATTERSON, Dan; PEAT, Andrew, James; POWERS, Jeremiah; PRICE, Daniel, J.; ROBERTS, Chris; TAI, Vincent; YOUNGMAN, Michael; WO2011/50284; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,76003-29-7

To a solution of 50.0 mmol of 5 and 60.0 mmol of 7 in 50.0 mL of 1,4-dioxane was added 0.500 mmol of copper (I) iodide followed by the addition of 100 mmol of K3P04 and 5 mmol of trans-cyclohexanediamine, then the resulting mixture was stirred at 100C for 16 h. The reaction mixture was cooled to rt and diluted with 500 mL of H20. The resulting aqueous solution was extracted with CHC13. The organic phase was washed with saturated NaCl, dried over MgS04 and concentrated in vacuo. The crude product was purified by column chromatography to give 43.4 mmol of 8. 4.2 Results [0176] Analytical data for exemplary compounds of structure 8 are provided below. 4.2.a tert-Butvl 4-(6-aminop_vridin-3-vl)-3-oxopiperazine-I -carboxvlate [0177] ‘H NMR (400 MHz, CDC13) No. 7.97-8.00 (m, 1H), 7.35-7.40 (m, 1H), 6.50-6.54 (m, 1H), 4.54 (br s, 2H), 4.24 (s, 2H), 3.65-3.69 (m, 2H), 3.75-3.80 (m, 2H), 1.50 (s, 9H); MS m/z: 293 (M+1).

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference：
Patent; ICAGEN, INC.; ASTELLAS PHARMA INC.; WO2005/99711; (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.

To a solution of 50.0 mmol of 5 and 60.0 mmol of 7 in 50.0 mL of 1,4-dioxane was added 0.500 mmol of copper (I) iodide followed by the addition of 100 mmol of K3P04 and 5 mmol of trans-cyclohexanediamine, then the resulting mixture was stirred at 100 C for 16 h. The reaction mixture was cooled to room temperature and diluted with 500 mL of H20. The resulting aqueous solution was extracted with CHC13. The organic phase was washed with saturated NaCl, dried over MgS04 and concentrated in vacuo. The crude product was purified by column chromatography to give 43.4 mmol of 8. ?H NMR (400 MHz, CDCl3) No. 7.97-8.00 (m, 1H), 7.35-7.40 (m, 1H), 6.50-6.54 (m, 1H), 4.54 (br s, 2H), 4.24 (s, 2H), 3.65-3.69 (m, 2H), 3.75-3.80 (m, 2H), 1.50 (s, 9H) ; MS m/z: 293 (M+1)., 76003-29-7

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ICAGEN, INC.; ASTELLAS PHARMA INC.; WO2005/100349; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To solution of tert-butyl 3-oxopiperazine-1-carboxylate (1.00 g) in dimethylformamide (20 ml) was added at 0C sodium hydride (240 mg) in three portions and stirring was continued at22C for 30 mm. (2-Bromoethoxy)(tert-butyl)dimethylsilane (1.43 g) was added at 0C andstirring was continued at 22C for 4 h. The mixture was partitioned between water and ethylacetate, the organic layer was dried, evaporated and the residue purified by flashchromatography (silica gel, 0 – 5% methanol in dichloromethane) to give the title compound(6.85 g) as a light yellow oil.MS (ESI, m/z): 359.2 [(M+H)], 76003-29-7

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

Reference：
Patent; SAVIRA PHARMACEUTICALS GMBH; EUROPEAN MOLECULAR BIOLOGY LABORATORY; LERNER, Christian; KREIS, Lukas; WEIKERT, Robert James; NEIDHART, Werner; HILPERT, Hans; (97 pag.)WO2017/158147; (2017); 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.

76003-29-7, To a solution of the product of Step 7 (10.0 g, 50.0 mmol) in anhydrous DMF(250 ml) in an ice-water bath were added sodium hydride (2.40 g, 60.0 mmol) andbenzyl chloride (6.60 g, 52.5 mmol). The mixture was stirred at RT for 4.5 h. Thereaction was quenched with water (10 ml), diluted with CH2CI2 (500 ml), and washedwith water (2x250ml). The organic layer was extracted with saturated NH4CI (200 ml),dried (MgSO4), concentrated, and purified by column chromatography (gradientMeOH/CH2CI2 0-5%) to give the product (10.7 g, 74%). 1H-NMR (CDCI3): 6=7.2-7.3(m, 5H), 4.57 (s, 2H), 4.10 (s, 2H), 3.53 (m, 2H), 3.19 (m, 2H), 1.41 (s, 9H).

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference：
Patent; SCHERING CORPORATION; WO2006/14944; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics