Tag: M.W:100-200

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.

59702-07-7, To the mixture of 450 mg 1-methylpiperazin-2-one (3.00 mmol) and 1.00 g K2C03 (7.24 mmol) in 5 mL TI-IF I mL 2-bromoethanol (14. Immol) was added and the mixture was stirred at 65¡ãC for 16h. The mixture was cooled to room temperature, filtered andconcentrated under reduced pressure. The residue was purified via flash chromatography using DCM and MeOH to give 4-(2-hydroxyethyl)-1-methyl-piperazin-2-one.MS: (M+H) 159.4.

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

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

300 mg mixture of 2,6-dichloro-4-[4-chloro-6-(4-fluorophenyl)thieno[2,3-Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; SZLAVIK, Zoltan; KOTSCHY, Andras; CHANRION, Maia; DEMARLES, Didier; GENESTE, Olivier; DAVIDSON, James Edward Paul; MURRAY, James Brooke; SIPOS, Szabolcs; PACZAL, Attila; BALINT, Balazs; (74 pag.)WO2016/207225; (2016); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

5317-33-9, To a solution of 3-N-(4-methylpiperazinyl)propan-1-ol (8.81 mmol, 1.39 g) in THF (40 ML) under N2 was added sodium metal (13.2 mmol, 0.30 g). The resulting suspension was stirred at 20 C. for 2 hours and then cannulated into a solution of 4-[(3-bromophenyl)amino]-7-fluoro-6-nitroquinazoline [J Med Chem, 1996(39):918] (0.80 g, 2.20 mmol) in THF (30 mL) under N2. Identical reaction procedure and workup as in the previous example gave, after chromatography on silica gel eluting with MeOH/CH2Cl2/EtOAc (1:9:10) to MeOH/CH2Cl2/EtOAc (2:3:5), 4-[(3-bromophenyl)amino)-7-[3-N-(4-methylpiperazinyl)propyloxy]-6-nitroquinazoline (0.36 g, 33%) as a yellow powder, mp (trihydrochloride salt) (MeOH/Et2O) 233 C. (dec). 1H NMR (free base, (CD3)2SO]: delta 10.12 (s, 1H, NH), 9.24 (s, 1H, H5), 8.69 (s, 1H, H2), 8.19 (br s, 1H, H-2′), 7.88 (br d, J=7.8 Hz, 1H, H-6′), 7.47 (s, 1H, H8), 7.38 (t, J=7.8 Hz, 1H, H-5′), 7.34 (dt, Jd=8.0, Jt=1.3 Hz, 1H, H-4′), 4.33 (t, J=6.1 Hz, 2H, CH2CH2CH2O), 2.45 (t, J=7.0 Hz, 2H, NCH2CH2CH2), 2.42-2.29 (br s, 8H, piperazinyl methylene), 2.15 (s, 3H, CH3N), 1.92 (quintet, J=6.7 Hz, 2H, CH2CH2CH2). Analysis calculated for C22H25BrN6O3.3HCl.H2O requires: C, 42.0; H, 4.8; N, 13.4; Cl, 16.9%. Found: C, 42.1; H, 4.5; N, 13.3; Cl, 16.9%.

5317-33-9 3-(4-Methylpiperazin-1-yl)propan-1-ol 79208, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Warner-Lambert Company; US6344459; (2002); B1;,
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

c. 5-tert-Butyl-2-{4-[2-(4-methyl-piperazin-1-yl)-ethoxy]-phenyl}-2H-pyrazol-3-ylamine (Intermediate 13c) To a solution of Intermediate 13b (1.15 g, 5.0 mmol), 2-(4-methyl-piperazin-1-yl)-ethanol (864 mg, 6.0 mmol), and triphenylphosphine (2.62 g, 10.0 mmol) in THF (10 mL), was added diisopropyl azodicarboxylate (2.0 g, 10.0 mmol) dropwise and stirred for 75 min. The mixture was diluted with diethyl ether (50 mL) and extracted with 10percent aqueous citric acid soln (2*). The combined aqueous layers were basified with solid potassium carbonate until pH=9. The aqueous layer was then extracted with ethyl acetate (3*). The combined ethyl acetate layers were washed with brine, dried (NaSO4) and evaporated in vacuo. Purification by FCC using 0-12percent [9:1 MeOH/880 ammonia] in DCM. The resulting product was crystallised (diethyl ether) to give the title compound (270 mg, 0.756 mmol, 15percent). LCMS (Method 1): Rt 2.31, 1.72 min, m/z 358/359 [MH+].

5464-12-0, Big data shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; Chiesi Farmaceutici S.p.A.; Van Niel, Monique Bodil; Ray, Nicholas Charles; Cridland, Andrew Peter; Hurley, Christopher; Alcaraz, Lilian; Panchal, Terry Aaron; Jennings, Andrew Stephen Robert; Armani, Elisabetta; US2013/150361; (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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

59702-07-7, To a vial were added methyl 6-bromoisoquinoline-3-carboxylate (83 mg, 0.31 mmol), 1- methylpiperazin-2-one (85 mg, 0.74 mmol), potassium phosphate, tribasic (175 mg, 0.81 mmol) and dioxane (2.5mL). The mixture was degassed by sparging with argon, RuPhos palladacycle Gen 4 pre-catalyst (22 mg, 8 mol%) was added and the vial was sealed and stirred at 100 C overnight. The reaction mixture was filtered, collected solids washed with EtOAc and purified on Si02 (0-10% methanol/dichloromethane) to give titled compound titled compound (20 mg 16%) as a yellow solid.

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

Reference£º
Patent; NURIX THERAPEUTICS, INC.; BARSANTI, Paul A.; BENCE, Neil F.; GOSLING, Jennifa; SAHA, Anjanabha; TAHERBHOY, Asad M.; ZAPF, Christoph W.; BOYLE, Kathleen; CARDOZO, Mario; MIHALIC, Jeffrey; LAWRENZ, Morgan; GALLOP, Mark; BRUFFEY, Jilliane; CUMMINS, Thomas; ROBBINS, Daniel; TANAKA, Hiroko; WANG, Chenbo; COHEN, Frederick; PALMER, Wylie; SANDS, Arthur T.; SHUNATONA, Hunter; (968 pag.)WO2019/148005; (2019); A1;,
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Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-fluorobenzonitrile (0.041 mol, 5 g) in DMF (10 ml) were added K2C03 (0.082 mol, 11.4 g) and 1 -methylpiperazine (0.062 mol, 6.15 g). The mixture was stirred over 1 8h at 100C. The mixture was partitioned between water and ethyl acetate. The organic phase was washed with water and brine. The resulting solution was dried oversodium sulfate and evaporated to dryness. The title compound was obtained as a white solid and used without further purification (7 g, 84%).(ESI+) MS: m/z 202.3 (MHj., 109-01-3

As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Patent; EUDENDRON S.R.L.; UNIVERSITA’ DEGLI STUDI DI MILANO; ANGIOLINI, Mauro; ZUCCOTTO, Fabio; BERNARDI, Anna; AIRAGHI, Francesco; (144 pag.)WO2016/96709; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

184042-60-2, 1-(2-Fluoroethyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 7-oxa-10,13,17,18,21 -pentaazatetracyclo[12.5.2.1A{2,6}.0A{17,20}]docosa- 1 (20),2,4,6(22),14(21 ),-15,18-heptaene hydrochloride (300 mg, 0.904 mmol) and diisopropylethylamine (616 muIota, 3.62 mmol) in tetrahydrofuran (2.5 ml) and N,N-dimethylformamide (2.5 ml) was added drop wise to a solution of di(imidazol- 1 -yl)methanone (220 mg, 1 .356 mmol) in tetrahydrofuran (1 .5 ml). The mixture was stirred at room temperature for 2 hours. 1 -(2-Fluoroethyl)piperazine hydrochloride (229 mg, 1 .36 mmol) was added and the reaction mixture was stirred at 80 C for 63 hours and at 1 10C for 24 hours. Di(imidazol-1 -yl)methanone (150 mg, 0.904 mmol) was added and the mixture was stirred at 1 10 0 C for 18 hours. The solvent was removed under reduced pressure and the residue was purified by reversed phase HPLC (HPLC method A). The product fractions were collected and the solvent was removed under reduced pressure. The product was taken up in dichloromethane/methanol (4:1 , 520 muIota) and 4N HCI in 1 ,4-dioxane (48 muIota, 0.191 mmol) was added. The reaction mixture was stirred at room temperature for 2 hours. The solvent was removed under reduced pressure and the compound was triturated with diethyl ether, filtered and dried under vacuum.Yield: 84 mg of example 17 (19%)LCMS method 2: MH+ = 454, RT = 2.032 min

184042-60-2, 184042-60-2 1-(2-Fluoroethyl)piperazine hydrochloride 22281452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; IPSEN PHARMA S.A.S.; ONCODESIGN S.A.; HOFLACK, Jan; BLOM, Petra; WO2013/46029; (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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, To a stirred and cooled (0 C.) solution of 2-bromoacetyl bromide (1.72 mL, 19.8 mmol) in dichloromethane (25 mL) was added a solution of tert-butyl piperazine-1-carboxylate (7.75 g, 41.6 mmol) in dichloromethane (20 mL), dropwise over ?20 minutes. The cooling bath was then removed and the reaction was allowed to stir another two hours before transferring to a separatory funnel along with a dichloromethane rinse of the reaction flask (?30 mL). The solution was washed with 1.0 N hydrochloric acid (2*?50 mL) and aqueous sodium bicarbonate solution (1*?50 mL). The organic layer was dried (Na2SO4) and concentrated to afford title compound as a clear, faint amber gum (5.68 g, 93%). The crude intermediate was deemed sufficiently pure to use, without purification, in the next step. 1H NMR (400 MHz, CDCl3) delta 3.87 (s, 2H), 3.63-3.57 (m, 2H), 3.55-3.41 (m, 6H), 1.48 (s, 9H) ppm.

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GENZYME CORPORATION; LIM, Sungtaek; BARKER, JR., Robert H.; CROMWELL, Mary A.; MAKINO, Elina; HIRTH, Bradford; JIANG, John; MANIAR, Sachin; MUNSON, Mark; CHOI, Yong-Mi; THURAIRATNAM, Sukanthini; MUSICK, Kwon Yon; PRIBISH, James; ANGELASTRO, Michael; US2020/102324; (2020); 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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

To a cooled solution of imidazole at 000 (1.00 g, 14.7 mmol, 2equiv) in 0H2012 (18 mL),benzyl chloroformate (1.03 mL, 7.35 mmol, 1 equiv) was slowly added. After 1h45 ofstirring the white solid (imidazole hydrochloride) was filtered off. The obtained filtrate wasconcentrated, and then solubilised in ethanol (17.5 mL). In another flask the solution ofpiperazine dihydrochloride (1.75 g, 11.03 mmol, 1.5 equiv) in water (17.5 mL) wasprepared, then added dropwisely to ethanolic solution of Cbz-imidazole. The resultedmixture was stirred for 4h30 at room temperature and then concentrated to 1h of itsvolume. Obtained aqueous phase was extracted with chloroform (4x) to remove the diacylated product, then NaOHsat was added to the previous aqueous phase (pH 9-10).The resulted aqueous phase was extracted again with chloroform (4x) to recover the monoacylated product. The organic phase with monoacylated product was washed with water (4x), dried over MgSO4 and concentrated to give (1) (0.809 g, 50% in two steps) asa colorless oil

142-64-3, As the paragraph descriping shows that 142-64-3 is playing an increasingly important role.

Reference£º
Patent; CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE; UNIVERSITE D’ORLEANS; AGROFOGLIO, Luigi; ROY, Vincent; PLEBANEK, Elzbieta; BESSIERES, Maxime; (105 pag.)WO2018/50771; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A reaction mixture of 8 (0.235 g, 1.0 mmol), l-(2,4-difluorophenyl)piperazine (0.208 g, 1.1 mmol), Pd(OAc)2 (28.8 mg, 0.13 mmol), BINAP (0.135 g, 0.22 mmol), and CS2CO3 (0.427 g, 1.3 mol) in dry toluene (5 mL) was stirred at 50 C for 48 h. After cooling, the palladium catalyst was removed by filtration through Celite pad. The product mixture was diluted with ethyl acetate (50 mL) and washed with aqueous NaHCCte (10 mL x 2) and brine (10 mL x 2). The organic layer was dried over magnesium sulfate, filtered, and concentrated in vacuo. The resulting product was purified by flash chromatography to yield 9 as a white solid (0.252 g, 0.72 mmol, 72%); Rf = 0.36 (20% ethyl acetate in hexane). NMR (400 MHz, CDCb) delta 7.83 (t, J = 8.8 Hz, 1H), 6.95 – 6.87 (m, 1H), 6.86 – 6.76 (m, 2H), 6.65 (dd, J = 9.0, 2.5 Hz, 1H), 6.54 (dd, J = 14.6, 2.5 Hz, 1H), 3.86 (s, 3H), 3.49 – 3.41 (m, 4H), 3.13 (dd, J = 6.2, 4.0 Hz, 4H). 13C NMR (101 MHz, CDCb) delta 165.09, 164.93, 164.89, 162.53, 159.53, 159.42, 157.1 1, 157.06, 157.00, 156.95, 155.53, 155.42, 154.59, 154.47, 136.30, 136.26, 136.21, 136.17, 133.44, 133.41, 119.80, 1 19.76, 1 19.71, 119.67, 1 1 1.02, 1 10.99, 1 10.81, 1 10.78, 109.50, 109.48, 107.70, 107.60, 105.16, 104.92, 104.90, 104.66, 101.75, 101.48, 77.16, 51.84, 50.60, 50.57, 47.43. MS (ESI) m/z 351 [M+H]+., 115761-79-0

The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; THE SCRIPPS RESEARCH INSTITUTE; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; ROUSH, William R.; CHOI, Jun Yong; PODUST, Larissa; WO2015/48306; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics