Month: February 2021

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

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

55276-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

(S)-Epichlorohydrin (48.0 mL, 0.612 mol) was added to a stirred solution of piperazine sulfonamide (87.3 g, 0.532 mol) in ethanol (1.33 L) at room temperature. The reaction mixture was stirred for 18 h and the white solid precipitate which formed was collected by filtration and washed with ethanol to afford the title intermediate (107.76 g) as a white solid which was used without further purification. (m/z): [M+H]+ calcd for C8H17ClN2O3S, 257.07; found 257.2. 1H NMR (DMSO-d6): delta (ppm) 2.37 (dd, 1H), 2.45 (dd, 1H), 2.50-2.58 (m, 4H), 2.86 (s, 3H), 3.09 (m, 4H), 3.55 (dd, 1H), 3.65 (dd, 1H), 3.84 (m, 1H), 5.09 (d, 1H).

The synthetic route of 55276-43-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; THERAVANCE, INC.; US2006/135764; (2006); 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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

In a nitrogen atmosphere, 115 mL of di-tert-butyl dicarbonate was dropwise added to chloroform (500 mL) solution of 50.0 g of (R)-2-methylpiperazine, over 1 hour. The reaction liquid was washed with water, and dried with anhydrous magnesium sulfate. The solvent was evaporated off under reduced pressure, and the residue was separated and purified through silica gel column chromatography (hexane/ethyl acetate = 2/1) to obtain 63.5 g of the entitled compound as a colorless oily substance., 75336-86-6

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BANYU PHARMACEUTICAL CO., LTD.; EP1726590; (2006); A1;,
Piperazine – Wikipedia
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

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;,
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.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of (3S ,5R)-tert-butyl 3,5 -dimethylpiperazine- 1 -carboxylate (2.1 4g, 10.0 mmol), 3-bromopropan-1-ol (2.76 g, 20 mmol) and K2C03(2.76 g, 20 mmol) in DMF (5.0 mL) was heated to 90C for 2 h in a microwave. The reaction mixture was poured into water (30 mL) and extracted with EtOAc. The organic phase was separated, dried and concentrated. The residue was purified by chromatography (DCM:MeOH=30: 1) to provide (3R,5S)-tert-butyl 4-(3- hydroxypropyl)-3 ,5 -dimethylpiperazine- 1 -carboxylate as a yellow liquid (2.1 4g, 50%)., 129779-30-2

129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PRINCIPIA BIOPHARMA, INC.; VERNER, Erik; BRAMELD, Kenneth Albert; WO2015/120049; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-31-7, 1-Ethylpiperazine-2,3-dione is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-31-7, 100 mg (0.32 mmol) of 5,5′-diallyl-3- (chloromethyl)-[1,1′-biphenyl] -2,2′-diol (Intermediate 4),54mg (0.38mmol) of N-ethyl-2,3-diketopiperazine,140.44mg (0.43mmol) of cesium carbonate, a catalytic amount of potassium iodide was added to a 10ml round bottom flask, acetonitrile was added to dissolve, heated to 80 C, and reacted overnight. After the reaction was completed, the reaction solution was cooled to room temperature, and then poured into water. Extracted with ethyl acetate, washed with saturated brine, dried over anhydrous sodium sulfate, spin-dried, and passed through a column (dichloromethane-methanol = 20/1) to obtain 42 mg of a yellow powdery solid with a yield of 31.1%.

As the paragraph descriping shows that 59702-31-7 is playing an increasingly important role.

Reference£º
Patent; Sichuan University; Chen Lijuan; Wei Yuquan; Ye Haoyu; (42 pag.)CN110343033; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

54699-92-2, 4-Methyl-1-piperazineacetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,54699-92-2

Example 13; General Method for the Preparation of Active Esters of N-Substituted Piperazine Acetic Acid from Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH2-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

The synthetic route of 54699-92-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Applera Corporation.; US2005/148771; (2005); A1;; ; Patent; Applera Corporation.; US2005/148774; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,934-98-5

[0498] The product was obtained analogously to intermediate product 22 starting from 2-(4-methyl-piperazin-1-yl)-ethylamine and 1-fluoro-2-nitro-benzene and after the addition of 15 mL of 5 M HCl in isopropanol isolated as the trihydrochloride salt. [0499] Yield: 72percent of theory [0500] ESI-MS: (M+H)+=235

As the paragraph descriping shows that 934-98-5 is playing an increasingly important role.

Reference£º
Patent; Boehringer ingelheim Pharma GmbH & Co.; US2003/236282; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics