Category: 70261-81-3

70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-81-3, 8.5 g (36.2 mmol) of crude I-a, 2.0 g of FeO(OH)/C catalyst and 100 mL of 95% ethanol were added to a 500 mL one-necked flask, and the mixture was heated under reflux, and a mixture of 25 mL of hydrazine hydrate and 20 mL of 95% ethanol was slowly added dropwise. The disappearance of the starting material by TLC (methanol: chloroform = 1:15). The filter cake was washed twice with hot ethanol (30 mL × 2). The solvent was evaporated under reduced pressure to give a white solid. Vacuum drying (I-a’) 6.7 g, The yield was 90.3%. The product was directly fed to the next reaction without further purification.

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shanghai Fuxing Pharmaceutical Industrial Co., Ltd.; Lu Shuai; Jin Qiaomei; Wang Yue; Chen Yadong; Lu Tao; (54 pag.)CN104592251; (2019); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

11 g (2.35 g, 10 mmol) was dissolved in a methanol solvent,Under nitrogen protection, 200 mg of Pd / C was added,And then through the H2 reaction,6h after the reaction is complete.The filtrate was collected by filtration, and concentrated to give 1.89 g of a solid. Yield 92%., 70261-81-3

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Nantong University; Ling, Yong; Mou, Jiefei; Xu, Qibing; Feng, Jiao; Zhu, Peng; Liu, Ji; Wang, Tingting; Ge, Xiang; Liang, Shanshan; (26 pag.)CN106432235; (2017); A;,
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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

General Procedure 3-1 : Synthesis of (4-((4-methylpiperazin-l-yl)methyl)aniline)[00187] The synthesis of the title compound was conducted as described in U.S. Pat. Appl. Publ.No. 2006058341 (March 16, 2006). Specifically, to a solution of 4-nitrobenzyl chloride in THF at the room temperature was added 1 -methyl piperazine. The solution was stirred for 3 hours after which time the crude reaction was diluted with ethyl acetate and washed repeatedly with water. The dried organics were concentrated to give directly the 4-nitrobenzylamine adduct.This was subsequently treated with Rainey Nickel in THF at 75PSI for 12 hours to give the title compound., 70261-81-3

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BIOGEN IDEC MA INC.; WO2008/94575; (2008); 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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, 8.5 g (36.2 mmol) of crude I-a, 2.0 g of FeO(OH)/C catalyst and 100 mL of 95% ethanol were added to a 500 mL one-necked flask, and the mixture was heated under reflux, and a mixture of 25 mL of hydrazine hydrate and 20 mL of 95% ethanol was slowly added dropwise. The disappearance of the starting material by TLC (methanol: chloroform = 1:15). The filter cake was washed twice with hot ethanol (30 mL ¡Á 2). The solvent was evaporated under reduced pressure to give a white solid. Vacuum drying (I-a’) 6.7 g, The yield was 90.3%. The product was directly fed to the next reaction without further purification.

The synthetic route of 70261-81-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shanghai Fuxing Pharmaceutical Industrial Co., Ltd.; Lu Shuai; Jin Qiaomei; Wang Yue; Chen Yadong; Lu Tao; (54 pag.)CN104592251; (2019); B;,
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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, To the 500 mL single neck flask was added 8.5 g (36.2 mmol) of crude I-a,FeO (OH) / C catalyst 2.0 g and 95% ethanol 100 mL,Heating reflux,A mixture of 25 mL of hydrazine hydrate and 20 mL of 95% ethanol was slowly added dropwise,TLC detects the disappearance of the starting material (methanol: chloroform = 1:15).The filter cake was washed twice with hot ethanol (30 mL x 2)The solvent was evaporated under reduced pressure to give a white solid,And dried in vacuo to give 6.7 g of (I-b) in a yield of 90.3%.Products without further purification, directly into the next step.

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; China Pharmaceutical University; Lu Shuai; Wang Yue; Zhi Yanle; Yao Chao; Lu Tao; Li Baoquan; Chen Puzhou; Bao Jiyin; (27 pag.)CN107245073; (2017); A;,
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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, EXAMPLE 3 4-((4-methyl-1-piperazinyl)methyl)aniline (I-c) Crude I-a (8.5g, 36.2mmol), FeO(OH)/C, 2.0 g as catalyst and 95% ethanol (100 ml) were added into a 500 mL single neck flask, which was refluxed. Into the reaction system were added slowly and dropwise a mixture of 25 mL hydrazine hydrate and 20 mL 95% ethanol. The depletion of the starting materials was confirmed by TLC (methanol: chloroform = 1:15). Suction filtration was performed while the reaction mixture was hot. The filter cake was washed with hot ethanol twice (30 ml *2). After removal of the solvent under reduced pressure, white solid was obtained, which was dried under vacuum to give 6.7 g (I-c); Yield: 90.3%. The product was used for subsequent reaction without further purification. 1H-NMR[300MHz, DMSO-d6]: delta2.1 (3H, s, -CH3), 2.3-2.5 (8H, m, -CH2-*4), 3.5 (2H, s, -CH2-), 4.0(2H, s, -NH2), 7.5 (2H, d, J = 8.7 Hz, ArH), 8.1 (2H, d, J = 8.7 Hz, ArH).

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Patent; China Pharmaceutical University; LU, Tao; WANG, Yue; CHEN, Yadong; LU, Yi; WANG, Zhanwei; JIN, Qiaomei; YANG, Taotao; LIN, Guowu; GUO, Qinglong; ZHAO, Li; EP2955185; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3,70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 4-Nitrobenzyl bromide (46.3mmol) was dissolved in dichloromethane (100mL). The solution was added to the mixture of relative amine (47.0mmol) and triethylamine (70.3mmol) in dichloromethane (20ml). The reaction mixture was stirred at r. t. for 24 h and was extracted with dichloromethane (100ml¡Á3). After removal of the solvent, the residue was crystallized from ethanol, giving yellow powder. Compounds 1 and 2 were used for further reaction without purification. To a suspension of compounds 1-2 (36.2mmol) in 95% ethanol (100ml), 85% NH2NH2¡¤H2O (362mmol), 95% ethanol (100ml) and iron (III) oxide hydroxide (FeO(OH)/C, 2.0g) were added and heated to reflux. When TLC analysis showed complete conversion of the starting material, the reaction mixture was filtrate through Cellit and the filtrate was concentrated in vacuum. The crude product was purified by silica gel colum chromatography (DCM/MeOH) to yield the title compound (3 and 4) as white solid. The mixture of compound 4 (1eq, 18.5mmol), 4-Nitro-1H-pyrazole-3-acid (1.1equiv, 20.4mmol), EDC (1.2equiv, 22.2mmol), HOBT (1.2equiv, 22.2mmol) in DMF (50ml) was stirred for 24h. The ice water (100ml) was added to the reaction mixture. A large amount of yellow solid precipitation (compound 8) was acquired. Compound 8 was used without further purification. Compounds 8 was reduced by the same process as compound 4, and then the resulting compound 12 was purified by column chromatography on silica gel, eluted with the appropriate solvent.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Article; Zhi, Yanle; Li, Baoquan; Yao, Chao; Li, Hongmei; Chen, Puzhou; Bao, Jiyin; Qin, Tianren; Wang, Yue; Lu, Tao; Lu, Shuai; European Journal of Medicinal Chemistry; vol. 155; (2018); p. 303 – 315;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-81-3, A mixture of 1-methyl-4-(4-nitro-benzyl)-piperazine (3.09 g, 13.1 mmol), zinc dust (4.29 g, 65.6 mmol) and ammonium chloride (2.81 g, 52.5 mmol) in methanol (100 mL) was refluxed 1h, cooled, filtered through Celite (washing with methanol) and evaporated to provide 4-(4-methyl-piperazin-1-ylmethyl)-phenylamine (2.67 g, 99% yield) as a pale yellow, waxy solid. 1H-NMR (DMSO-d6, 500 MHz) 6.89 (d, 2H), 6.49 (d, 2H), 4.89 (s, 2H), 3.24 (s, 2H), 2.3 (br m, 8H) ppm; MS (FIA) 206.2 (M+H); HPLC (Method A) co-elutes with solvent front.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2004/46120; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-81-3, General procedure: These amines were required for the syntheses of 4 and 20 respectively. To a solution of 4-nitrobenzylchloride (1 mmol) in anhydrous THF (3 mL) was added 1-methylpiperazine or piperidine (1 mmol) and triethylamine (1.5 mmol, 0.21 mL). The solution was heated at 70 C overnight. The reaction mixture was then extracted with dichloromethane and water. The organic fractions were combined, dried over anhydrous Na2SO4, and concentrated under reduced pressure. The residue was purified by column chromatography (hexane/EA 1:4) and characterized by 1H NMR (Supplementary Information). It was dissolved in 10 mL ethanol, PtO2 (0.01 g) was added under nitrogen. Hydrogenation was carried out on a Parr hydrogenator at 50 psi for 16 h. The catalyst was then removed by filtration and the filtrate was concentrated in vacuo to give the amine in quantitative yield.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Article; Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 2917 – 2929;,
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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.,70261-81-3

A mixture of 1-methyl-4-(4-nitro-benzyl)-piperazine (3.09 g, 13.1 mmol), zinc dust (4.29 g, 65.6 mmol) and ammonium chloride (2.81 g, 52.5 mmol) in methanol (100 mL) was refluxed 1h, cooled, filtered through Celite (washing with methanol) and evaporated to provide 4-(4-methyl-piperazin-1-ylmethyl)-phenylamine (2.67 g, 99% yield) as a pale yellow, waxy solid. 1H-NMR (DMSO-d6, 500 MHz) 6.89 (d, 2H), 6.49 (d, 2H), 4.89 (s, 2H), 3.24 (s, 2H), 2.3 (br m, 8H) ppm; MS (FIA) 206.2 (M+H); HPLC (Method A) co-elutes with solvent front.

The synthetic route of 70261-81-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2004/46120; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics