14 Sep 2021 News Brief introduction of 4-Methylpiperazin-2-one

34770-60-0, The synthetic route of 34770-60-0 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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

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. 6.1.17 4-Methyl-1-(5-vinylpyridin-2-yl)piperazin-2-one (14b) A mixture of 2-bromo-5-vinylpyridine 3b (0.15 g, 0.81 mmol), 4-methylpiperazin-2-one (0.18 g, 1.63 mmol), N,N’-dimethylethylene diamine (0.007 g, 0.08 mmol), K2CO3 (0.22 g, 1.63 mmol) and CuI (0.007 g, 0.04 mmol) in anhydrous toluene was heated to reflux and the reaction was continued as described in general procedure IV to afford 14b (0.11 g) in 62.8% yield. 1H NMR (400 MHz, CDCl3): delta 8.40 (d, J = 2.3 Hz, 1H), 8.12 (dd, J = 8.6, 1.0 Hz, 1H), 7.80 (dd, J = 8.7, 2.4 Hz, 1H), 6.72 (dd, J = 17.7, 11.0 Hz, 1H), 5.81 (dd, J = 17.7, 0.7 Hz, 1H), 5.38 (dd, J = 11.0, 0.8 Hz, 1H), 3.66-3.76 (m, 2H), 3.28 (s, 2H), 2.76-2.82 (m, 2H), 2.41 (s, 3H); LC-MS: 218 (M++1).

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

Reference:
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

14 Sep 2021 News Brief introduction of 4-Methylpiperazin-2-one

34770-60-0, The synthetic route of 34770-60-0 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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

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. 6.1.17 4-Methyl-1-(5-vinylpyridin-2-yl)piperazin-2-one (14b) A mixture of 2-bromo-5-vinylpyridine 3b (0.15 g, 0.81 mmol), 4-methylpiperazin-2-one (0.18 g, 1.63 mmol), N,N’-dimethylethylene diamine (0.007 g, 0.08 mmol), K2CO3 (0.22 g, 1.63 mmol) and CuI (0.007 g, 0.04 mmol) in anhydrous toluene was heated to reflux and the reaction was continued as described in general procedure IV to afford 14b (0.11 g) in 62.8% yield. 1H NMR (400 MHz, CDCl3): delta 8.40 (d, J = 2.3 Hz, 1H), 8.12 (dd, J = 8.6, 1.0 Hz, 1H), 7.80 (dd, J = 8.7, 2.4 Hz, 1H), 6.72 (dd, J = 17.7, 11.0 Hz, 1H), 5.81 (dd, J = 17.7, 0.7 Hz, 1H), 5.38 (dd, J = 11.0, 0.8 Hz, 1H), 3.66-3.76 (m, 2H), 3.28 (s, 2H), 2.76-2.82 (m, 2H), 2.41 (s, 3H); LC-MS: 218 (M++1).

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

Reference:
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

14 Sep 2021 News Brief introduction of 4-Methylpiperazin-2-one

34770-60-0, The synthetic route of 34770-60-0 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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

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. 6.1.17 4-Methyl-1-(5-vinylpyridin-2-yl)piperazin-2-one (14b) A mixture of 2-bromo-5-vinylpyridine 3b (0.15 g, 0.81 mmol), 4-methylpiperazin-2-one (0.18 g, 1.63 mmol), N,N’-dimethylethylene diamine (0.007 g, 0.08 mmol), K2CO3 (0.22 g, 1.63 mmol) and CuI (0.007 g, 0.04 mmol) in anhydrous toluene was heated to reflux and the reaction was continued as described in general procedure IV to afford 14b (0.11 g) in 62.8% yield. 1H NMR (400 MHz, CDCl3): delta 8.40 (d, J = 2.3 Hz, 1H), 8.12 (dd, J = 8.6, 1.0 Hz, 1H), 7.80 (dd, J = 8.7, 2.4 Hz, 1H), 6.72 (dd, J = 17.7, 11.0 Hz, 1H), 5.81 (dd, J = 17.7, 0.7 Hz, 1H), 5.38 (dd, J = 11.0, 0.8 Hz, 1H), 3.66-3.76 (m, 2H), 3.28 (s, 2H), 2.76-2.82 (m, 2H), 2.41 (s, 3H); LC-MS: 218 (M++1).

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

Reference:
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

Simple exploration of 34770-60-0

34770-60-0 4-Methylpiperazin-2-one 13704283, 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.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×3), and the organic phase was washed with saturated brine (20 mL×2). 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:
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

Some tips on 34770-60-0

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

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:
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

New learning discoveries about 4-Methylpiperazin-2-one

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

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

Some tips on 34770-60-0

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

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:
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

New learning discoveries about 4-Methylpiperazin-2-one

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

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

Simple exploration of 34770-60-0

34770-60-0 4-Methylpiperazin-2-one 13704283, 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.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×3), and the organic phase was washed with saturated brine (20 mL×2). 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:
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

Some tips on 34770-60-0

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

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:
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