Category: 34770-60-0

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The reaction conditions for 1-4.3.28 differ: Under argon atmosphere 1-2.2 (250 mg, 0.54 mmol), potassium carbonate (150 mg, 1.07 mmol), copper (I) iodide (10 mg, 0.05 mmol), Nu,Nu’- dimethylethylendiamine (25 L, 0.23 mmol) and 4-methyl-piperazin-2-one (75 mg, 0.66 mmol) in dioxane (10 mL) are heated to 80 C for 8 d. The reaction mixture is filtered and the solution is concentrated. The residue is purified by reversed phase HPLC. Yield 30%, m/z 500 [M+H]+, rt 0.98 min, LC-MS Method V011 S01.

34770-60-0, As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; ANDERSKEWITZ, Ralf; GRAUERT, Matthias; GRUNDL, Marc; HAEBEL, Peter, Wilhelm; OOST, Thorsten; PAUTSCH, Alexander; PETERS, Stefan; BINDER, Florian; VINTONYAK, Viktor; WO2014/140075; (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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

( v) 1 -(4- ( [2-Amino-4-(butylamino )-6-methylpyrimidin-5-yl]methyl } -3-methoxyphenyl)-4- methylpiperazin-2-oneTo a solution of of the product from step (iv) (0.144 g, 0.380 mmol) in 1 ,4-dioxane (2 mL) was added Cul (72.0 mg, 0.379 mmol), N,N’-dimethyldiaminoethane (0.0820 mL, 0.763 mmol), 4-methylpiperazin-2-one (87.0 mg, 0.760 mmol), and Cs2C03 (247 mg, 0.760 mmol). The mixture was heated to 100C and stirred for 1 Oh. After cooling, water was added and the resulting mixture was extracted with EtOAc. The combined organic solutions were washed with brine, and then dried (Na2S04). After removal of the solvent in vacuo, the crude residue was purified by silica gel column chromatography to give the title compound as a pale yellow solid (120 mg, 0.291 mmol, 77 %); 1H NMR: 6.90 (1H , d), 6.86 (1H, s,), 6.72 (1H, d), 4.76 (3H, br s), 3.87 (3H, s), 3.68-3.65 (2H, m), 3.63 (2H, s,), 3.32-3.27 (2H, m), 3.26 (2H, s), 2.78-2.75 (2H, m), 2.39 (3H, s), 2.27 (3H, s), 1.45-1.37 (2H, m), 1.26-1.19 (2H, m), 0.85 (3H, t); LC-MS: m/z = 413 [MH+] (T = 1.48 min).

34770-60-0, 34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Dainippon Sumitomo Pharma Co., Ltd.; ASTRAZENECA AKTIEBOLAG; TOSAKI, Shinya; HORI, Seiji; WO2012/67268; (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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

( v) 1 -(4- ( [2-Amino-4-(butylamino )-6-methylpyrimidin-5-yl]methyl } -3-methoxyphenyl)-4- methylpiperazin-2-oneTo a solution of of the product from step (iv) (0.144 g, 0.380 mmol) in 1 ,4-dioxane (2 mL) was added Cul (72.0 mg, 0.379 mmol), N,N’-dimethyldiaminoethane (0.0820 mL, 0.763 mmol), 4-methylpiperazin-2-one (87.0 mg, 0.760 mmol), and Cs2C03 (247 mg, 0.760 mmol). The mixture was heated to 100C and stirred for 1 Oh. After cooling, water was added and the resulting mixture was extracted with EtOAc. The combined organic solutions were washed with brine, and then dried (Na2S04). After removal of the solvent in vacuo, the crude residue was purified by silica gel column chromatography to give the title compound as a pale yellow solid (120 mg, 0.291 mmol, 77 %); 1H NMR: 6.90 (1H , d), 6.86 (1H, s,), 6.72 (1H, d), 4.76 (3H, br s), 3.87 (3H, s), 3.68-3.65 (2H, m), 3.63 (2H, s,), 3.32-3.27 (2H, m), 3.26 (2H, s), 2.78-2.75 (2H, m), 2.39 (3H, s), 2.27 (3H, s), 1.45-1.37 (2H, m), 1.26-1.19 (2H, m), 0.85 (3H, t); LC-MS: m/z = 413 [MH+] (T = 1.48 min).

34770-60-0, 34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Dainippon Sumitomo Pharma Co., Ltd.; ASTRAZENECA AKTIEBOLAG; TOSAKI, Shinya; HORI, Seiji; WO2012/67268; (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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

mixture of 4-methyl-2-piperazinone (200 mg, 1.75 mmol), 4-iodoaniline (384 mg, 1.75 mmol), K3PO4 (848 mg, 4.00 mmol) and 1,2-trans-diaminocyclohexane (98 uL, 0.80 mmol) in dioxane (6 mL) was degassed with Ar before being charged with CuI (76 mg, 0.40 mmol). The mixture in a sealed tube was heated at 110 0C for 4 h. It was then purified by a silica gel prep-TLC using CH2C12/MeOH (95/5) as solvents to give the desired product (25 mg). MS 206.2 (M+H)., 34770-60-0

The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PORTOLA PHARMACEUTICALS, INC.; WO2006/55951; (2006); 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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

34770-60-0, Compounds t-butyl-(5-(bromomethyl)-6-(dimethoxymethylpyrid-2-yl)(methyl) aminocarboxylate 15a (70 mg, 0.19 mmol), 174 4-methylpiperazin-2-one (43 mg, 0.38 mmol), 52 sodium hydride (19 mg, 0.47 mmol, 60% 53 mineral oil mixture) and 99 N,N-dimethyl formamide (3 mL) were mixed, and stirred for 1 h at room temperature. This mixture was quenched with 9 water, extracted with dichloromethane (20 mL¡Á3), and the organic phase was washed with saturated brine (20 mL¡Á2). The organic phase was dried over anhydrous sodium sulfate, and filtered to remove the drying agent. The residuals were purified through a preparative silica gel plate (petroleum ether/ethyl acetate 1.5:1), to obtain the target 175 product t-butyl-(6-(dimethoxymethyl)-5-((4-methyl-2-carbonylpiperazin-1-yl)methyl) pyrid-2-yl)(methyl) aminocarboxylate 15b (60 mg, colorless solid), at a yield of 83%. (0274) MS m/z (ESI): 409 [M+1].

34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Nanjing InnoCare Pharma Tech Co., Ltd.; KONG, Norman Xianglong; ZHOU, Chao; ZHENG, Zhixiang; US2019/144427; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(i) 2-Methoxy-4-(4-methyl-2-oxopiperazin-l-yl) benzaldehvde To a solution of 4-bromo-2-methoxybezaldehyde (10.0 g, 46.5 mmol) in 1 ,4-dioxane (140 mL) was added Cul (8.84 g, 46.5 mmol), N,N’-dimethyldiaminoethane (10.0 mL, 93.0 mmol), 4-methylpiperazin-2-one (7.95 g, 69.8 mmol), and Cs2C03 (45.0 g, 139 mmol). The mixture was heated to 100C and stirred for 5h. After cooling, the mixture was filtered, and the solution was adjusted to pH 2~3 with IN HCl. After stirring for 3h at r.t., the mixture was neutralized with sat. aq. NaHC03,and the resulting mixture was extracted with EtOAc. The combined organic solutions were washed with brine, and then dried (Na2S04). After removal of the solvent in vacuo, the subtitle compound was obtained as a white solid (10.7 g, 43.1 mmol, 93%); NMR: 10.4 (1H, s), 7.86 (1H, d), 7.1 1 (1 H, d), 6.92 (1H, dd), 3.92 (3H, s),3.76 (2H, t), 3.30 (2H, s), 2.82 (2H, t), 2.42 (3H, s); LC-MS: m/z = 249 [MH+] (T = 0.92 min).

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Dainippon Sumitomo Pharma Co., Ltd.; ASTRAZENECA AKTIEBOLAG; TOSAKI, Shinya; HORI, Seiji; WO2012/67268; (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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

Step A: To a solution of 4-bromo-benzaldehyde (1.8 g, 9.73 mmol), 4-methylpiperazine-2-one (1.44 g, 12.6 mmol), Pd2(dba)3 (768 mg, 0.84 mmol), Xantphos (435 mg, 0.75 mmol) and cesium carbonate (5.48 g, 16.8 mmol) in dioxan (30 mL) was added water (1 drop). The mixture was stirred under nitrogen atmosphere at 90C for 1.5 h. After cooling, the mixture was filtered. The filtrate was concentrated to dryness under vacuum. The residue was purified with silica gel chromatography to give 4-(4-methyl-2-oxopiperazine-1-yl)benzaldehyde(1.8 g, 84.8%) as white solid. MS(ESI)m/z:219[M+H+].

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chai Tai Tianqing Pharmaceutical Group Co., Ltd.; DING, Zhaozhong; WU, Hao; SUN, Fei; WU, Lifang; YANG, Ling; (60 pag.)EP3190113; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3-14-2 Preparation of 1-(2-Amino-1-(3-methoxy-4-((6-methoxypyridin-3-yl)methoxy)benzyl)-1H-benzo[d]imidazol-5-yl)-4-methylpiperazin-2-one To a stirred suspension of 5-iodo-1-(3-methoxy-4-((6-methoxypyridin-3-yl)methoxy)benzyl)-1H-benzo[d]imidazol-2-amine (0.25 g, 0.48 mmol) in 1,4-dioxane (8 mL) was added 4-methylpiperazin-2-one (0.11 g, 0.96 mmol), CuI (0.036 mg, 0.19 mmol), trans-N,N’-dimethylcyclohexane-1,2-diamine (0.044 g, 0.38 mmol), and tribasic potassium phosphate (0.32 g, 1.52 mmol). The mixture was heated to 145 C. in a microwave reactor. After 3 h, the mixture was allowed to cool to room temperature and was filtrated through Celite. The filtrate was concentrated, and the residue was purified by silica gel chromatography (2-5% methanol/dichloromethane elute) followed by prep-HPLC to afford 0.030 g (12%) of the product as a white solid: 1H NMR (500 MHz, CDCl3) delta 8.17 (s, 1H), 7.66 (dd, J=8.0, 2.0 Hz, 1H), 7.25 (s, 1H), 7.01 (d, J=8.0 Hz, 1H), 6.86 (d, J=8.0 Hz, 1H), 6.79 (d, J=8.0 Hz, 1H), 6.76-6.74 (m, 2H), 6.64 (d, J=7.5 Hz, 1H), 4.99 (s, 2H), 4.89 (br s, 2H), 4.81 (s, 2H), 3.94 (s, 3H), 3.79 (s, 3H), 3.72 (t, J=5.0 Hz, 2H), 3.30 (s, 2H), 2.82 (t, J=5.0 Hz, 2H), 2.44 (s, 3H) ppm; (M+1)=503., 34770-60-0

34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; KANE, JR., John L.; MATTHEWS, Gloria; METZ, Markus; KOTHE, Michael; LIU, Jinyu; SCHOLTE, Andrew; US2015/158847; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 6.1.15. General procedure IV, for preparation of 14a-f A mixture of aryl bromide (1.0 mmol), 4-methylpiperazin-2-one (for compounds 15-17)/morpholin-3-one (for compounds 18-20) (2.0 mmol), N,N0-dimethylethylene diamine (0.1 mmol), K2CO3 (2.0 mmol) and CuI (0.05 mmol) in anhydrous toluene was heated to reflux with stirring for 6 h. Then the reaction mixture was cooled to room temperature, poured into water, stirred vigorously and extracted thrice with ethyl acetate, dried over anhydrous Na2SO4, concentrated under reduced pressure and purified by flash chromatography to afford compounds 14a-f in 54-68% yields. 6.1.18 1-(2-Fluoro-4-vinylphenyl)-4-methylpiperazin-2-one (14c) A mixture of 1-bromo-2-fluoro-4-vinylbenzene 3c (0.2 g, 0.99 mmol), 4-methylpiperazin-2-one (0.22 g, 1.99 mmol), N,N’-dimethylethylene diamine (0.008 g, 0.09 mmol), K2CO3 (0.27 g, 1.99 mmol) and CuI (0.009 g, 0.04 mmol) in anhydrous toluene was heated to reflux and the reaction was continued as described in general procedure IV to afford 14c (0.12 g) in 55% yield. 1H NMR (400 MHz, CDCl3): delta 7.18-7.24 (m, 3H), 6.66 (dd, J = 17.5, 10.8 Hz, 1H), 5.74 (d, J = 17.5 Hz, 1H), 5.32 (d, J = 10.8 Hz, 1H), 3.62-3.69 (m, 2H), 3.30 (s, 2H), 2.77-2.84 (m, 2H), 2.42 (s, 3H); LC-MS: 235 (M++1)., 34770-60-0

34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Rakesh; Bruhn, David; Maddox, Marcus; Lee, Robin B.; Yang, Lei; Lee, Richard E.; Madhura, Dora B.; Trivedi, Ashit; Meibohm, Bernd; Scherman, Michael S.; Gilliland, Janet C.; Gruppo, Veronica; McNeil, Michael R.; Lenaerts, Anne J.; Bioorganic and medicinal chemistry; vol. 20; 20; (2012); p. 6063 – 6072,10;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[00249] 5A: l-(isoquinolin-5-yl)-4-methylpiperazin-2-one: To 5-bromoisoquinoline (1.657 g, 7.96 mmol) and 4-methylpiperazin-2-one (1, 8.76 mmol) was added DMSO (7 mL), 1,10-phenanthroline (0.144 g, 0.796 mmol), potassium carbonate (3.30 g, 23.89 mmol) and the mixture was degassed with Ar for 30 min. Copper(I)iodide (1.213 g, 6.37 mmol) was added and the reaction was heated in oil bath at 130 C overnight. The reaction was cooled to room temperature and quenched with NH4OH (10 mL) and water (20 mL) and diluted with EtOAc. The aqueous layer was extracted EtOAc (2 x 50 mL) and then, nBuOH (lx 30 mL). Combined organic layers were washed with brine and dried (MgS04). Purification by silica gel chromatography afforded 1.5g ( 78%) yellow solid. MS (ESI) m/z: 242.0 (M+H)+.

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; PINTO, Donald J.P.; CLARK, Charles G.; ORWAT, Michael J.; SMITH II, Leon M.; EWING, William R.; WO2014/59202; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics