Tag: M.W:100-200

74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

74879-18-8, Intermediate 16 (3S)-3-Meth l-1 -{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine(2S)-2-Methylpiperazine (15 g, 150 mmol) was dissolved in tetrahydrofuran (300 mL) and the solution was cooled down to 0C. Sodium hydroxide (150 mL, 449 mmol) was added, then 4-(trifluoromethyl)benzenesulfonyl chloride (40 g, 164 mmol) (dissolved in 200ml THF) was added dropwise and the resulting mixture was stirred for 1 h. Further 4-(trifluoromethyl)benzenesulfonyl chloride (0.06eq , 2.2g) was added and mixture stirred for 10 min. The mixture was diluted with DCM (500ml) and water (500ml) and stirred for 5 min. The phases were separated, the aqueous layer was extracted with DCM (1000ml) and the organic phases concentrated under reduced pressure. The residue was taken-up with 1 M HCI (500ml) and washed with DCM in order to extracted impurities. The aqueous phase was basified to pH=9 with NaOH 3M, extracted with DCM ( 3x 500ml) and the combined organic phases dried over Na2S04 before the solvent was removed under reduced pressure to give the title compound (30 g).LCMS (low pH) m/z (ES) 309 [M+H]+ 1 H NMR (400 MHz, CDCI3) delta 1 .06 (d, J = 7.2 Hz, 3H), 1.94 (t, J = 10.4 Hz, 1 H), (td, J = 1 1 .2, 4.0 Hz, 1 H), 2.88-3.07 (m, 3H), 3.66 (m, 2H), 7.83 (d, J = 8.4 Hz, 2H), 7.90 (d, J = 8.4 Hz, 2H) ppm

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference：
Patent; CONVERGENCE PHARMACEUTICALS LIMITED; HEER, Jag Paul; CRIDLAND, Andrew Peter; NORTON, David; WO2011/86377; (2011); 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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

10.0 g 2-chloro-3 -methyl-4-(4,4, 5,5 -tetramethyl- 1,3 ,2-dioxaborolan-2-yl)phenol(Preparation 5a) (37.2 mmol), 8.7 g 2-(4-methylpiperazin-1-yl)ethanol (60.3 mmol) and15.8 g PPh3 (60.3 mrnol) were dissolved in 100 mL dry toluene and then 27 mL diethylazodicarboxylate (60.3 mmol, 40percent solution in toluene) was added dropwise. The mixturewas stirred at 50°C under argon for 1.5 hours. The volatiles were evaporated under reducedpressure and 100 rnL Et20 was added. The precipitated white crystals were filtered off and washed with Et20. The filtrate was concentrated under reduced pressure and pudfied via flash chromatography using CHC13 and MeOH as eluents. The resulting light brown oil was crystallized from hexanc to give Preparation Sb as an off-white solid.?11 NMR (500 MHz, DMSO-d6): 7.56 (d, 111), 6.99 (d, 1H), 4.15 (t, 2H), 2.72 (t, 2H), 2.51 (s, 311), 2.50 (br s, 4H), 2.29 (br s, 411), 2.13 (s, 311), 1.29 (s, 12H)., 5464-12-0

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; KOTSCHY, Andras; SZLAVIK, Zoltan; CSEKEI, Marton; PACZAL, Attila; SZABO, Zoltan; SIPOS, Szabolcs; RADICS, Gabor; PROSZENYAK, Agnes; BALINT, Balazs; BRUNO, Alain; GENESTE, Olivier; DAVIDSON, James Edward Paul; MURRAY, James Brooke; CHEN, I-Jen; PERRON-SIERRA, Francoise; WO2015/97123; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

75336-86-6, Intermediate 26:; (3R)-3-methyl-l-[4-(methylsulfonyl)phenyl]piperazine; A mixture of 4-fluorophenyl methyl sulfone (2.00 g), (R)-2-methylpiperazine (2.30 g) and K2CO3 (3.20 g) in anhydrous DMF (80 mL) was heated at 100°C for 5 hours. The reaction mixture was filtered to remove salts and the solvent was evaporated under reduced pressure to give a yellow oil. Purification by flash chromatography (CHCls/MeOH) gave 1.36 g (47percent) of the title compound as a pale yellow solid. M^SI): 255.2. HPLC (Condition A), Rt: 1.0 min (HPLC purity: 100 percent).

As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference：
Patent; Applied Research Systems ARS Holding N.V.; WO2006/10751; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5464-12-0

1.91 g 4-bromo-3-fluoro-phcnol (10.0 mmol), 1.73 g 2-(4-methylpiperazin-1 -yl)ethanol(12.0 mmol) and 5.00 g immobilized PPh3 (15.0 mrnol) were dissolved in 30 mL drytoluene under N2, then 2.99 g diterrbutyl azodicarboxylate (13.0 mmol) was added and themixture was stirred at 50°C for 6 hours. Then it was filtered, the filtrate was concentrated under reduced pressure and purified via flash chromatography using EtOAc and MeOll as eluents to obtain I -[2-(4-bromo-3 -fluoro-phenoxy)ethyl] -4-methyl-piperazine.MS (M+H): 317.2.

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; KOTSCHY, Andras; SZLAVIK, Zoltan; CSEKEI, Marton; PACZAL, Attila; SZABO, Zoltan; SIPOS, Szabolcs; RADICS, Gabor; PROSZENYAK, Agnes; BALINT, Balazs; BRUNO, Alain; GENESTE, Olivier; DAVIDSON, James Edward Paul; MURRAY, James Brooke; CHEN, I-Jen; PERRON-SIERRA, Francoise; WO2015/97123; (2015); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

PREPARATION 6 2-(4-Methyl-1-piperazinyl)ethanol 2-Chloroethanol (36.0 g, 30 mL, 0.44 mol) was added to 1-methylpiperazine (27.0 g, 30 mL, 0.27 mol) and potassium carbonate (40 g, 0.29 mol) in acetonitrile (100 mL) with stirring. The reaction mixture was heated under reflux for 48 h, then filtered, and the solids were washed with acetonitrile. The combined filtrates were evaporated under reduced pressure and the resulting oil was distilled at 12 mm Hg to give the title compound (31 g, 0.21 mol) as a light tan oil. Electrospray MS m/z 145 [M+H]+.

109-01-3, The synthetic route of 109-01-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Astra Aktiebolag; US6218538; (2001); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of Intermediate 9 (500 mg, 1.48 mmol) in NMP (6 mL) were added (cyclopropyl)(piperazin-l-yl)methanone (455 mg, 2.95 mmol) and DIPEA (1.3 mL), and the mixture was heated at 140C for 16 h. The reaction mixture was taken up in EtOAc^ (150 mL) and water (50 mL) and the organic layer was washed with water (2 x 50 mL) and brine (50 mL). The organic layer was separated and dried (phase separation cartridge), and the solvent was removed in vacuo. Purification by columnchromatography (Si02, 10-20% EtOAc in isohexane) gave a beige solid (390 mg, 57%). To a solution of this material (390 mg, 0.85 mmol) in DCM (6 mL) was added TFA (3 mL) and the resulting solution was stirred at r.t. for 15 minutes. The solvents were30removed in vacuo. The residue was dissolved in MeOH (5 mL), then placed on an SCX cartridge, washed (MeOH), eluted (7M ammonia in MeOH) and concentrated in vacuo to afford a white solid (304 mg, 100%). To a portion of this material (60 mg, 0.17 mmol) in NMP (1.2 mL) were added DIPEA (0.14 mL) and 4-chloropyrido[3,2-c/]pyrimidine (33 – – mg, 0.2 mmol). The resulting solution was heated under microwave irradiation at 150C for 1 h. Purification by preparative HPLC afforded the title compound (51 mg, 61%) as a beige solid. deltaEta (DMSO-ifc) 8.93-8.88 (2H, m), 8.54 (2H, d, J 11.51 Hz), 8.17 (IH, dd, J 8.46, 1.58 Hz), 7.90 (IH, dd, J 8.46, 4.25 Hz), 7.74 (IH, dd, J 8.94, 6.26 Hz), 7.33 (IH, t, J9.12 Hz), 5.91 (IH, m), 4.05-3.13 (8H, s), 2.58 (3H, m), 2.12-2.07 (IH, m), 1.67 (3H, d, J 6.71 Hz), 0.90-0.73 (4H, m). LCMS (ES+) 486 (M+H)+, RT 2.78 minutes (Method 2).

59878-57-8, The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; UCB PHARMA S.A.; ALLEN, Daniel, Rees; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MATTEUCCI, Mizio; OWENS, Andrew, Pate; RAPHY, Gilles; SHARPE, Andrew; WO2011/58108; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5464-12-0, 10.0 g Preparation B2 (37.2 mmol), 8.7 g 2-(4-methylpiperazin-1-yl)ethanol (60.3 mmol) and 15.8 g PPh3 (60.3 mmol) were dissolved in 100 mL dry toluene and then 27 mL diethyl azodicarboxylate (60.3 mmol, 40 percent solution in toluene) was added dropwise. The mixture was stirred at 50 °C under argon until no further conversion was observed. The volatiles were evaporated under reduced pressure and 100 mL Et20 was added. Theprecipitated white crystals were filtered off and washed with Et20. The filtrate was concentrated under reduced pressure and purified via flash chromatography using CHC13 and MeOH as eluents. The resulting light brown oil was crystallized from hexane to give Preparation B4 as an off-white solid. 1H NMR (500 MHz, DMSO-d6) oe: 7.56 (d, 1H), 6.99 (d, 1H), 4.15 (t, 2H), 2.72 (t, 2H), 2.51 (s, 3H), 2.50 (br s, 4H), 2.29 (br s, 4H), 2.13(s, 3H), 1.29 (s, 12H)

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference：
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; SZLAVIK, Zoltan; SZABO, Zoltan; CSEKEI, Marton; PACZAL, Attila; KOTSCHY, Andras; BRUNO, Alain; GENESTE, Olivier; CHEN, I-Jen; DAVIDSON, James Edward Paul; MURRAY, James Brooke; ONDI, Levente; RADICS, Gabor; SIPOS, Szabolcs; PROSZENYAK, Agnes; PERRON-SIERRA, Francoise; BALINT, Balazs; (188 pag.)WO2016/207226; (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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

2-(4-Methylpiperazin-1-yl)ethyl 4-nitrophenyl carbonate To a stirred solution of 1-(2-hydroxyethyl)piperazine (26.0 g, 0.2 mol) in DMF (200 mL) was added formic acid (752 mL, 0.2 mol) and formaldehyde (16.2 g, 0.2 mol, 37% solution in water) The reaction mixture was cautiously heated at 100 C. for 2 hours then stirred overnight at room temperature. The solvent was removed in vacuo. This procedure was repeated 3 further times to give ~100 g of product. The crude products were combined and distilled under vacuum to give, at 74 C., 2-(4-methylpiperazin-1-yl)ethanol (51 g, 44%) as a colourless liquid. Analytical LCMS: (System C, RT=0.70 min), ES+: 145.1 [MH]+., 103-76-4

As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference：
Patent; Biovitrum AB; US2009/281087; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoic acid 54 (0.022 mmol), HATU (0.027 mmol) and l-methylpiperazin-2-one (0.022 mmol) are dissolved in dry DMF (0.5 mL) at rt. Diisopropylethylamine (0.06 mmol) is added to the solution. The reaction mixture is stirred for 1 h at rt. HPLC purification affords 4-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoyl)- l-methylpiperazin-2-one Gl as a TFA salt. 1H NMR (400MHz, J6-DMSO) delta 10.1 (s, IH), 8.87 (s, 2H), 7.90 (d, J = 8.4 Hz, 2H), 7.79 (d, J = 8.7 Hz, 2H), 7.43 (d, J = 8.4Hz, 2H), 7.29 (d, J = 8.0 Hz, 2H), 7.12 (t, J = 51.2 Hz, IH), 4.1 (s, 2H), 2.87 (s, 3H), 2.55 (m, 4H). MS (m/z) (M+l)+: 454.2., 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference：
Patent; IRM LLC; WO2009/26276; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics