Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

A heterogeneous mixture of methyl (E)-1-acetyl-3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate (25 g ), N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (22.4 g, for preparation, see e.g. US 6762180 Bl or US 8304541 B2), methanol (200 ml) and N,N-dimethylformamide (50 ml) was stirred and heated to reflux for 3-4 hours. A clear brown solution was obtained. A sample was drawn and analyzed for the presence of the limiting starting material (nmt 1 %). Piperidine (10.5 ml) was then added and the mixture was stirred under reflux for another 30-60 minutes. The product precipitated out during the stirring. The reaction mixture was analyzed for the intermediate and once nmt 1 % remained as determined by HPLC, the mixture was cooled to 0 C and stirred from 2 h to overnight. The solids were isolated by filtration and washed twice with methanol (75 ml per wash), then dried in a vacuum oven at 40 C overnight to obtain methyl (Z)-3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate (33.7 g, 88 %, 99.8 a-%) as a bright yellow solid., 262368-30-9

As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference£º
Patent; FERMION OY; PIISOLA, Antti; TOIS, Jan; (13 pag.)WO2019/97112; (2019); A1;,
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Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of intermediate 1.2 (4g) in MeCN (100ml_) were added (S)-1-Boc-2- hydroxymethylpiperazine (3.07g) and DIPEA (3.54ml_) at RT. The reaction mixture was stirred at 80C for 28h. After cooling down, the reaction mixture was diluted with EA and washed with water (2x) and brine. The aq. layers were extracted with EA. The combined org. layers were dried over MgS04, filtrated off and evaporated to dryness. The crude was purified by CC (Biotage, SNAP 340g, solvent A: Hep; solvent B: EA; gradient in %B: 30 over 3CV, 30 to 50 over 5CV, 50 over 3CV) to afford 4g of yellow foam. LC-MS (A): tR = 0.87min; [M+H]+: 426.0., 1030377-21-9

The synthetic route of 1030377-21-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; IDORSIA PHARMACEUTICALS LTD; CAROFF, Eva; MEYER, Emmanuel; (32 pag.)WO2018/11265; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,122833-04-9

5-chloro-N-(2-methoxy-4-(4-methyIpiperazin-l-yl)phenyl)-4-(3-nitrophenoxy)pyrimidin- 2-amine A flask was charged with 2,5-dichloro-4-(3-nitrophenoxy)pyrimidine (1.56 g, 5.45 mmol), 2-methoxy-4-(4-methylpiperazin-l-yl)benzenamine (1.21 g, 5.45 mmol), TFA ( 0.42 mL, 5.45 mmol uL), 2-BuOH (30 mL). The slurry was heated to 1000C for 2h. The reaction mixture was allowed to cool to room temperature and, was neutralized with a saturated aqueous sodium bicarbonate solution. The aqueous mixture was then extracted with ethyl acetate (50 mL) three times. The crude product was purified using flash chromatography with 30: 1 :0.3 (v/v/v) dichloromethane-methanol-triethylamine to afford 2.07 g brown solid (81%). 1H NMR 600 MHz (DMSO d6) delta 8.38 (s, IH), 8.28 (s, IH), 8.16 (m, 2H), 7.76 (m, 2H), 7.08 (s, I H), 6.46 (m, IH), 6.14 (m, I H), 3.72 (s, 3H), 3.33 (m, 4H), 3.05 (m, 4H), 2.28 (s, 3H); MS m/z: 471.91 (M+1).

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; DANA FARBER CANCER INSTITUTE; GRAY, Nathanael, S.; JANNE, Pasi; ECK, Michael, J.; ZHOU, Wenjun; WO2010/129053; (2010); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of l-[4-(trifluoromethyl)phenyl]piperazine (500 mg, 2.17 mmol). ethyl 2-bromoacetate (545 mg, 3.26 mmol), and DIEA (421 mg) in CH3CN (20 mL) was stirred for 2 h at RT. The resulting mixture was concentrated under vacuum. The residue was purified by silica gel column chromatography using EtOAc / petroleum ether (1/3) to afford 600 mg (87%) of the title compound as a colorless oil. LC-MS: (ES, m/z): 317.3

30459-17-7, 30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CENTAURUS THERAPEUTICS; ROMERO, Donna L.; MCCALL, John M.; BLITZER, Jeremy; (118 pag.)WO2018/112077; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step-2: To a solution of (E)-methyl 1-acetyl-3-(ethoxy(phenyl)methylene)-2-oxo-2,3-dihydro-1H-pyrrolo[3,2-c]pyridine-6-carboxylate (40 mg, 0.109 mmol) in DMF (0.2 mL) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (28 mg, 0.109 mmol) at room temperature, and the reaction mixture was stirred at 110 C. for 2 h. The reaction mixture was cooled to RT, piperidine (0.2 mL) was added and stirred for 10 minutes at room temperature. The solvent was evaporated and the resulting residue was purified by silica gel column chromatography using 5% CH3OH in dichloromethane as eluent to afford (Z)-methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxo-2,3-dihydro-1H-pyrrolo[3,2-c]pyridine-6-carboxylate as yellow solid. MS (ES+): m/z 541.3 (MH+).

262368-30-9, 262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ANGION BIOMEDICA CORP.; NARAYAN, Prakash; HUANG, Brian; PAKA, Prani; PAKA, Latha; GOLDBERG, Itzhak D.; US2015/105380; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

639068-43-2, tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

639068-43-2, 2) Synthesis of cis-1-tert-butoxycarbonyl-3,5-dimethyl-4-benzyl piperazine To a suspension of 10 g (46.66 mmol.) of cis-1-tert-butoxycarbonyl-3,5-dimethyl piperazine and 12.90 g (93.3 mmol.) of potassium carbonate in N,N-dimethylformamide (100 ml) was added, at room temperature, 11.97 g (70 mmol.) of benzyl bromide. The mixture was stirred for 16 hours at 120¡ã C. To the reaction system was added water, which was subjected to extraction with ethyl acetate. The organic layer was washed with a saturated aqueous saline solution, which was dried over magnesium sulfate, followed by distilling off the solvent. The residue was purified by means of a column chromatography (ethyl acetate/hexane 30percent) to give the object compound as a pale yellow oily product. The yield was 13.56 g (95percent). 1H-NMR (CDCl3, 200 MHz) delta: 1.04 (6H, d, J=5.8 Hz), 1.45 (9H, s), 2.45-2.75 (4H, m), 3.67-3.92 (2H, m), 3.81 (2H, s), 7.15-7.39 (5H, m). IR (neat): 2980, 1693, 1423, 1136, 1061, 924, 883, 766, 729, 700 cm-1.

639068-43-2 tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 22219990, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Takeda Chemical Industries, Ltd.; US6235731; (2001); B1;,
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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Intermediate 51 : (3-Methyl-piperazin- 1 -yl)-(l -m-tolyl- 1 H-[ 1 ,2,4]triazol-3-yl)-methanone 51.1 : 2-Methyl-4-(l-m-tolyl-lH-[l ,2,4]triazole-3-carbonyl)-piperazine-l-carboxylic acid tert- butyl ester 2.00 g (9.84 mmol) l-m-tolyl-lH-[l ,2,4]triazole-3-carboxylic acid was stirred with 3.30 g (10.3 mmol) TBTU and 2.50 mL (14.6 mmol) DIPEA in 30 mL DCM at RT. After 10 min, 2.05 g (9.84 mmol) 2-methyl-piperazine-l-carboxylic acid tert-butyl ester was added and the reaction mixture was stirred at RT for 12 h. The solvent was removed by distillation. The residue was taken up in water and extracted with EtOAc. The combined organic phases were dried over sodium sulfate, filtered and concentrated in vacuo. The crude material was purified by flash chromatography (EtOAc). Yield: 4.00 g (95 %), purity: 90% ESI-MS: m/z = 386 (M+H)+ Rt(HPLC) : 1.48 min (method 8)

120737-78-2, As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; WO2013/87805; (2013); 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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (300 mg, 1.5 mmol) , butyric acid (200 mg, 2.3 mmol) , EDCI (595 mg, 3.0 mmol) and HOAT (306 mg, 2.3 mmol) in DCM (10 mL) was stirred at 0 , and DIPEA (0.76 mL, 4.5 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 10 h and washed with water (10 mL ¡Á 3) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 4-butyryl-3-methylpiperazine-1-carboxylate as colorless liquid (370 mg, 91) .1H NMR (600 MHz, CDCl3) : delta ppm 4.74-4.81, 4.34-4.41 (m, 0.5H, 0.5H) , 3.80-4.12, 3.53-3.60 (m, 2.5H, 0.5H) , 3.26-3.35, 2.75-2.98 (m, 0.5H, 2.5H) , 2.26-2.35 (m, 2H) , 1.61-1.69 (m, 2H) , 1.47 (s, 9H) , 1.13-1.24 (m, 3H) , 1.12 (t, J 7.3 Hz, 3H) and MS-ESI: m/z 215.10 [M-55] +., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

60% Sodium hydride (154 mg, 3.85 mmol) was added portionwise to te/t-butyl (S)-3- (hydroxymethyl)piperazine-l-carboxylate (832 mg, 3.85 mmol) in THF (15 ml) cooled to 0C over a period of 5 minutes under nitrogen. The resulting mixture was stirred at 0C for 10 minutes then allowed to warm to room temperature and stirred for 20 minutes. 7-Bromo-8-chloro-5- fluoroquinazolin-4-ol (970 mg, 3.5 mmol) was added and the mixture heated at 65C and stirred for 2 hours then cooled to room temperature. Further 60% sodium hydride (154 mg, 3.85 mmol) was added and then heated at 65C and stirred for a further 2 hours before cooling to room temperature. The reaction mixture was diluted with EtOAc (100 ml), and water (25 ml). The aqueous phase was taken to pH 5 with acetic acid and separated. The aqueous phase was extracted with EtOAc (100 ml) and the organic phases combined, dried and evaporated. The residue was purified by flash silica chromatography, elution gradient 0 to 20% MeOH in DCM. Pure fractions were evaporated to dryness to afford te/t-butyl (S)-3-(((7-bromo-8-chloro-4-hydroxyquinazolin-5-yl)oxy)methyl)piperazine-l- carboxylate (1.35 mg, 82%) as pale yellow foam. 1H NM (500 M Hz, DMSO, 27C) 1.38 (9H, s), 2.53 – 2.68 (2H, m), 2.68 – 2.85 (2H, m), 2.85 – 2.97 (2H, m), 3.72 (1H, d), 3.87 – 3.99 (2H, m), 4.1 – 4.19 (1H, m), 7.38 (1H, s), 8.14 (1H, s). m/z: ES+ [M+H]+ 473., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; BOYD, Scott; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; RAUBO, Piotr, Antoni; (144 pag.)WO2018/206539; (2018); 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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

General procedure: The mixture of 2-amino-5-bromobenzoic acid (1.00 g,4.63 mmol), triethyl orthoformate (1.00 mL, 6.02 mmol), amine(6.02 mmol), iodine (0.12 g, 0.046 mmol) and anhydrous ethanol(20 mL) was refluxed under nitrogen atmosphere for 4-6 h, thenconcentrated under vacuum to give a residue which was dissolvedin ethyl acetate (90 mL). The ethyl acetate solution was washedwith 1 N aqueous sodium hydroxide (20 mL 3) and brine(30 mL 3), dried over anhydrous sodium sulfate and concentratedto give a white or light yellow solid.

70261-82-4, The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Zhang, Hao; Xin, Min-Hang; Xie, Xiao-Xiao; Mao, Shuai; Zuo, Sai-Jie; Lu, She-Min; Zhang, San-Qi; Bioorganic and Medicinal Chemistry; vol. 23; 24; (2015); p. 7765 – 7776;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics