Sep 2021 News New learning discoveries about 1-(2-Methoxyethyl)piperazine

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution containing 2.7 g (18.9 mmol) of 1-[2-(methyloxy)ethyl]piperazine and 20 ml. of THF at O0C was added 0.9 g (23 mmol) of a 60% suspension of NaH in mineral oil. The reaction mixture was allowed to stir for 15 min and 3.0 g (18.9 mmol) of 2- chloro-5-nitropyridine was added. The reaction mixture was heated at 6O0C overnight and then quenched by the addition of water and extracted with EtOAc. The combined organic layers were dried over MgSO4 and the solvents were removed under reduced pressure. The residue was subjected to silica gel chromatography to give 2.7 g (54%) of 1-[2-(methyloxy)ethyl]-4-(5-nitro-2-pyridinyl)piperazine as a yellow solid: 1H NMR (400 MHz, DMSO-d6) delta 2.50-2.53 (m, 6H), 3.24 (s, 3 H), 3.46 (t, J = 5.7 Hz, 2 H), 3.71 – 3.78 (m, 4 H), 6.94 (d, J = 9.7 Hz, 2 H), 8.21 (dd, J = 9.6 and 2.8 Hz, 1 H), and 8.95 (d, J = 2.75 Hz, 1 H)., 13484-40-7

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/32667; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News New learning discoveries about 1-(2-Methoxyethyl)piperazine

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution containing 2.7 g (18.9 mmol) of 1-[2-(methyloxy)ethyl]piperazine and 20 ml. of THF at O0C was added 0.9 g (23 mmol) of a 60% suspension of NaH in mineral oil. The reaction mixture was allowed to stir for 15 min and 3.0 g (18.9 mmol) of 2- chloro-5-nitropyridine was added. The reaction mixture was heated at 6O0C overnight and then quenched by the addition of water and extracted with EtOAc. The combined organic layers were dried over MgSO4 and the solvents were removed under reduced pressure. The residue was subjected to silica gel chromatography to give 2.7 g (54%) of 1-[2-(methyloxy)ethyl]-4-(5-nitro-2-pyridinyl)piperazine as a yellow solid: 1H NMR (400 MHz, DMSO-d6) delta 2.50-2.53 (m, 6H), 3.24 (s, 3 H), 3.46 (t, J = 5.7 Hz, 2 H), 3.71 – 3.78 (m, 4 H), 6.94 (d, J = 9.7 Hz, 2 H), 8.21 (dd, J = 9.6 and 2.8 Hz, 1 H), and 8.95 (d, J = 2.75 Hz, 1 H)., 13484-40-7

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/32667; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13 Sep 2021 News Brief introduction of 1-(2-Methoxyethyl)piperazine

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a mixture of 5-cyclopropyl-5-phenyl- (0.01 mol; 1) or 5-cyclopropyl-5-(4-chlorophenyl)-imidazolidine-2,4-dione (0.01 mol; 2), 40% solution of formaldehyde (0.01 mol) in 96% ethanol (20 mL), corresponding 4-substituted piperazines (0.01 mol), tetrahydroisoquinoline (THIQ) or morpholine dissolved in 96% ethanol (10 mL) were added. The mixture was left for ca. 12 h at room temperature and then refrigerated at ca. -10 C for 24 h. The precipitated crude products were washed with cold ethanol, separated by filtration and recrystallized from 96% ethanol.

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Byrtus, Hanna; Obniska, Jolanta; Czopek, Anna; Kami?ski, Krzysztof; Paw?owski, MacIej; Bioorganic and Medicinal Chemistry; vol. 19; 20; (2011); p. 6149 – 6156;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News New learning discoveries about 1-(2-Methoxyethyl)piperazine

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

A solution of (i?)-3-(6-(2- fluorophenyl)-5,6-dihydrobenzo[h]quinazolin-2-ylamino)phenethyl methanesulfonate (5.37 g, 11.00 mmol), l-(2-methoxyethyl)piperazine (3.32 niL, 22.34 mmol) and triethylamine (1.5 niL, 11.17 mmol) in JV,JV-dimethylacetamide (30 mL) was heated at 90 0C for 20 h. After cooling to room temperature, water (200 mL) was added while stirring. The suspension was stirred for 15 min. and filtered. Solid was taken into dichloromethane (200 mL), dried over sodium sulfate and concentrated. Product was purified by flash column chromatography on silica gel (120 g silica gel column, 0-10% 7N NH3 in methanol-dichloromethane, over 80 min.) to afford the title compound as a yellow solid (5.50 g, 93% yield). 1H-NMR (DMSO- d6): delta 9.53 (s, 1 H), 8.37-8.34 (m, 1 H), 8.33 (s, 1 H), 7.81 (s, 1 H), 7.62-7.60 (m, 1 H), 7.51- 7.46 (m, 2 H), 7.30-7.19 (m, 3 H), 7.08-7.02 (m, 2 H), 6.82-6.79 (m, 2 H), 4.67 (t, J= 7.2 Hz, 1 H), 3.41 (t, J= 5.6 Hz, 2 H), 3.22-3.08 (m, 2 H), 3.33 (s, 3 H), 2.74-2.70 (m, 2 H), 2.59- 2.42 (m, 12 H). LCMS m/e 539 [M+H].

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference:
Patent; ARQULE, INC.; ALI, Syed, M.; ASHWELL, Mark; TANDON, Manish; YANG, Rui-yang; LIU, Yanbin; VENSEL, David; EATHIRAJ, Sudharshan; PALMA, Rocio; LAPIERRE, Jean-marc; WESTLUND, Neil; WU, Hui; NAMDEV, Nivedita; KELLEHER, Eoin; KELLEHER, Eugene; WO2010/78421; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News New learning discoveries about 1-(2-Methoxyethyl)piperazine

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

A solution of (i?)-3-(6-(2- fluorophenyl)-5,6-dihydrobenzo[h]quinazolin-2-ylamino)phenethyl methanesulfonate (5.37 g, 11.00 mmol), l-(2-methoxyethyl)piperazine (3.32 niL, 22.34 mmol) and triethylamine (1.5 niL, 11.17 mmol) in JV,JV-dimethylacetamide (30 mL) was heated at 90 0C for 20 h. After cooling to room temperature, water (200 mL) was added while stirring. The suspension was stirred for 15 min. and filtered. Solid was taken into dichloromethane (200 mL), dried over sodium sulfate and concentrated. Product was purified by flash column chromatography on silica gel (120 g silica gel column, 0-10% 7N NH3 in methanol-dichloromethane, over 80 min.) to afford the title compound as a yellow solid (5.50 g, 93% yield). 1H-NMR (DMSO- d6): delta 9.53 (s, 1 H), 8.37-8.34 (m, 1 H), 8.33 (s, 1 H), 7.81 (s, 1 H), 7.62-7.60 (m, 1 H), 7.51- 7.46 (m, 2 H), 7.30-7.19 (m, 3 H), 7.08-7.02 (m, 2 H), 6.82-6.79 (m, 2 H), 4.67 (t, J= 7.2 Hz, 1 H), 3.41 (t, J= 5.6 Hz, 2 H), 3.22-3.08 (m, 2 H), 3.33 (s, 3 H), 2.74-2.70 (m, 2 H), 2.59- 2.42 (m, 12 H). LCMS m/e 539 [M+H].

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference:
Patent; ARQULE, INC.; ALI, Syed, M.; ASHWELL, Mark; TANDON, Manish; YANG, Rui-yang; LIU, Yanbin; VENSEL, David; EATHIRAJ, Sudharshan; PALMA, Rocio; LAPIERRE, Jean-marc; WESTLUND, Neil; WU, Hui; NAMDEV, Nivedita; KELLEHER, Eoin; KELLEHER, Eugene; WO2010/78421; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 1-(2-Methoxyethyl)piperazine

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution containing 2 7g (18 9 mmol) of 1-[2-(methyloxy)ethyl]piotaperaziotane and 20 mL of THF at O0C was added 0 9 g (23 mmol) of a 60% suspension of sodium hydride in mineral oil The reaction mixture was allowed to stir for 15 mm and 3 O g (18 9 mmol) of 2-chloro-5-niotatropyriotadiotane was added The reaction mixture was heated at 60 0C overnight and then quenched by the addition of H2O and extracted with EtOAc The combined organic layers were dried over MgSO4 and the solvents were removed under reduced pressure The residue was subjected to silica gel chromatography to give 2 7g (54%) of 1-[2-(methyloxy)ethyl]-4-(5-niotatro-2- pyriotadiotanyl)piotaperaziotane as a yellow solid 1 H-NMR (400 MHz, DMSO-cfe) delta 8 95 (d, J = 2 8 Hz, 1 H), 8 21 (dd, J = 9 6 and 2 8 Hz, 1 H), 6 94 (d, J = 9 7 Hz, 2 H), 3 71 – 3 78 (m, 4 H), 3 46 (t, J = 5 7 Hz, 2 H), 3 24 (s, 3 H), and 2 50 – 2 53 (m, 6 H)

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; GLAXOSMITHKLINE LLC; ADJABENG, George; BAUM, Erich; BIFULCO, Neil; DAVIS-WARD, Ronda, G.; DICKERSON, Scott, Howard; DONALDSON, Kelly, Horne; HORNBERGER, Keith; PETROV, Kimberly; RHEAULT, Tara, Renae; SAMMOND, Douglas, McCord; SCHAAF, Gregory, M.; STELLWAGEN, John; UEHLING, David, Edward; WATERSON, Alex, Gregory; WO2010/104899; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 1-(2-Methoxyethyl)piperazine

13484-40-7, 13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, 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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

Synthesis of N-[3-(4-{[4-(2-methoxyethyl)piperazinyI]methyl}phenyl)-4- oxoindeno[2,3-d]pyrazol-5-yl](morpholin-4-ylamino)carboxamide dihydrochloride (compound B16):Acetic acid (5.76 g, 96 mmole) was added to a suspension of aldehyde (10 g, 24 mmole) and piperazine (6.91 g, 48 mmole) in NMP (150 mL). The reaction was stirred at room temp for 16h then treated with NaB(OAc)3H (12.7 g, 60 mmole). The reaction was stirred at room temp for 2Oh during which time the reaction becomes very viscous. IN NaOH (200 mL) was then added and the reaction was stirred for Ih. The reaction was then poured onto H2O (750 mL) and filtered. The solid was washed with H2O (2 x 350 mL), EtOH (100 mL), and Et2O (200 mL). The solid was then dried under vacuum to yield the desired amine as the free base (9.98 g, 76%). The free base was then suspended in EtOH (200 mL) and heated to boiling. The suspension was then treated with 4N HCl in dioxane (15 mL). The suspension clears then after ~15 min, a thick precipitate forms. Additional EtOH (200 mL) was added to facilitate stirring. Once the suspension cooled to room temp, it was filtered and the solid was washed with EtOH (200 mL) and Et2O (200 mL). The solid was then dried under vacuum to yield the desired bis-hydrochloride salt (10.3 g) designated compound B 16.

13484-40-7, 13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; GPC BIOTECH, INC.; WO2006/2119; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 1-(2-Methoxyethyl)piperazine

13484-40-7, 13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, 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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

Synthesis of N-[3-(4-{[4-(2-methoxyethyl)piperazinyI]methyl}phenyl)-4- oxoindeno[2,3-d]pyrazol-5-yl](morpholin-4-ylamino)carboxamide dihydrochloride (compound B16):Acetic acid (5.76 g, 96 mmole) was added to a suspension of aldehyde (10 g, 24 mmole) and piperazine (6.91 g, 48 mmole) in NMP (150 mL). The reaction was stirred at room temp for 16h then treated with NaB(OAc)3H (12.7 g, 60 mmole). The reaction was stirred at room temp for 2Oh during which time the reaction becomes very viscous. IN NaOH (200 mL) was then added and the reaction was stirred for Ih. The reaction was then poured onto H2O (750 mL) and filtered. The solid was washed with H2O (2 x 350 mL), EtOH (100 mL), and Et2O (200 mL). The solid was then dried under vacuum to yield the desired amine as the free base (9.98 g, 76%). The free base was then suspended in EtOH (200 mL) and heated to boiling. The suspension was then treated with 4N HCl in dioxane (15 mL). The suspension clears then after ~15 min, a thick precipitate forms. Additional EtOH (200 mL) was added to facilitate stirring. Once the suspension cooled to room temp, it was filtered and the solid was washed with EtOH (200 mL) and Et2O (200 mL). The solid was then dried under vacuum to yield the desired bis-hydrochloride salt (10.3 g) designated compound B 16.

13484-40-7, 13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; GPC BIOTECH, INC.; WO2006/2119; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-(2-Methoxyethyl)piperazine

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-Chloro-IJ-{ 3- [5-fluoro-3- (4-methoxyphenyl) -4- oxo-8-propoxy-4H-quinolin-l-yl] propyl} acetamide (370 mg, 0.8 mmol) was suspended in acetonitrile (12 ml) . l-(2- Methoxyethyl)piperazine (138 mg, 0.96 mmol), triethylamine (162 mg, 1.6 mmol) and acetonitrile (2 ml) were added to the suspension, and stirred at 70 to 8O0C for 6 hours. The resulting mixture was concentrated under reduced pressure, and the residue was subjected to extraction using ethyl acetate. The extract was then sequentially washed with water, an aqueous saturated sodium chloride solution, and an aqueous saturated sodium bicarbonate solution. The washed product was concentrated under reduced pressure, and the residue was purified using silica gel column chromatography (dichloromethane : methanol = 30 : 1 ? 10 : 1) . The purified product was concentrated under reduced pressure, and the residue was then dissolved in ethyl acetate (5 ml) . A 4N hydrogen chloride ethyl acetate solution (0.19 ml) was added thereto and stirred, and then the mixture was concentrated to dryness under reduced pressure, giving a pale yellow amorphous solid of N-{ 3- [5-fluoro-3- (4-methoxyphenyl) -A- oxo-8-propoxy-4H-quinolin-l-yl] propyl} -2- [4- (2- methoxyethyl) piperazin-1-yl] acetamide hydrochloride (200 mg) .1H-NMR (DMSO-d6) deltappm: 1.00 (3H, t, J=7.3 Hz), 1.78-1.89 (4H, m) , 2.50-3.00 (4H, m) , 2.96-3.20 (8H, m) , 3.25 (3H, s), 3.62-3.66 (4H, m) , 3.75 (3H, s) , 3.98-4.04 (2H, m) , 4.56 (2H, t, J=6.4 Hz), 6.91-7.02 (3H, m) , 7.24 (IH, dd, J=4.5 Hz, 9.1 Hz), 7.60 (2H, d, J=8.8 Hz), 8.00 (IH, s) , 8.07 (IH, brs) .

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference:
Patent; OTSUKA PHARMACEUTICAL CO., LTD.; OTSUBO, Kenji; YAMAUCHI, Takahito; OCHI, Yuji; WO2010/64735; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-(2-Methoxyethyl)piperazine

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-Chloro-IJ-{ 3- [5-fluoro-3- (4-methoxyphenyl) -4- oxo-8-propoxy-4H-quinolin-l-yl] propyl} acetamide (370 mg, 0.8 mmol) was suspended in acetonitrile (12 ml) . l-(2- Methoxyethyl)piperazine (138 mg, 0.96 mmol), triethylamine (162 mg, 1.6 mmol) and acetonitrile (2 ml) were added to the suspension, and stirred at 70 to 8O0C for 6 hours. The resulting mixture was concentrated under reduced pressure, and the residue was subjected to extraction using ethyl acetate. The extract was then sequentially washed with water, an aqueous saturated sodium chloride solution, and an aqueous saturated sodium bicarbonate solution. The washed product was concentrated under reduced pressure, and the residue was purified using silica gel column chromatography (dichloromethane : methanol = 30 : 1 ? 10 : 1) . The purified product was concentrated under reduced pressure, and the residue was then dissolved in ethyl acetate (5 ml) . A 4N hydrogen chloride ethyl acetate solution (0.19 ml) was added thereto and stirred, and then the mixture was concentrated to dryness under reduced pressure, giving a pale yellow amorphous solid of N-{ 3- [5-fluoro-3- (4-methoxyphenyl) -A- oxo-8-propoxy-4H-quinolin-l-yl] propyl} -2- [4- (2- methoxyethyl) piperazin-1-yl] acetamide hydrochloride (200 mg) .1H-NMR (DMSO-d6) deltappm: 1.00 (3H, t, J=7.3 Hz), 1.78-1.89 (4H, m) , 2.50-3.00 (4H, m) , 2.96-3.20 (8H, m) , 3.25 (3H, s), 3.62-3.66 (4H, m) , 3.75 (3H, s) , 3.98-4.04 (2H, m) , 4.56 (2H, t, J=6.4 Hz), 6.91-7.02 (3H, m) , 7.24 (IH, dd, J=4.5 Hz, 9.1 Hz), 7.60 (2H, d, J=8.8 Hz), 8.00 (IH, s) , 8.07 (IH, brs) .

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference:
Patent; OTSUKA PHARMACEUTICAL CO., LTD.; OTSUBO, Kenji; YAMAUCHI, Takahito; OCHI, Yuji; WO2010/64735; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics