Category: piperazines

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

148 6-((3R.5SV3.5-Dimethyl-4-thiazol-2-ylmethyl-rhoirhoerazin-l-ylmethvn-2-(lH- indazol-4-yl)-4-morpholin-4- yl-thieno [3.2-d]p yrimidine.Via 2-chloro-6-((3R,5 S)-3 ,5 -dimethyl-4-thiazol-2-ylmethyl-piperazin- 1 – ylmethyl)-4-mophiholin-4-yl-thieno[3,2-d]pyrimidine, prepared from (2R,6S)-2,6- dimethyl- 1 -thiazol-2-ylmethyl-piperazine.Amine preparation: 2-Thiazolecarboxaldehyde was converted to the corresponding alcohol by treatment with sodium borohydride. Reaction with methanesulfonyl chloride yielded methanesulfonic acid thiazol-2-ylmethyl ester. A mixture of methanesulfonic acid thiazol-2-ylmethyl ester (393mg), (3R,5S)-3,5- dimethyl-piperazine-1 -carboxylic acid tert-butyl ester (described previously, 435mg), potassium carbonate (309mg) and tetrabutyl ammonium iodide (827mg) was heated to reflux in MeCN (1OmL). After 4 days the reaction mixture was cooled, diluted with ethyl acetate, washed with water and dried (MgSO4). The solvent was evaporated and the residue purified by flash chromatography to give (R)-3,5- dimethyl-4-thiazol-2-ylmethyl-piperazine-l -carboxylic acid (S) -tert-butyl ester (314mg). Treatment of this compound with HCl in DCM/MeOH yielded the desired amine, which was isolated as the hydrochloride salt. EPO 1H NMR (400MHz, CDCl3) 1.12 (d, J=6.0Hz, 6H), 2.06 (m, 2H), 2.85 (m, 4H), 3.80 (s, 2H), 3.92 (m, 4H), 4.09 (m, 4H), 4.17 (s, 2H), 7.24 (d, J=3.2Hz, IH), 7.38 (s, IH), 7.51 (m, IH), 7.59 (d, J=8.3Hz, IH), 7.74 (d, J=3.3Hz, IH), 8.29 (d, J=7.3Hz, IH), 9.03 (s, IH), 10.1 (br s, IH); MS (ESf) 561 (MH+)., 129779-30-2

As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference£º
Patent; PIRAMED LIMITED; WO2006/46031; (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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

314741-40-7, To a stirred solution of tert-butyl (3S)-3-(hydroxymethyl)piperazine-1-carboxylate (5.0 g, 23.1 mmol) and imidazole (2.36 g, 34.7 mmol) in DCM (25 ml) was added tert-butyl(chloro)dimethylsilane (3.59 g, 23.8 mmol). The reaction was stirred at ambient temperature for 72 hours. The reaction mixture was diluted with sat. aq. NaHCO3 (50 ml) and the organic layer separated. The aqueous layer was extracted with DCM (2¡Á30 ml), the combined organics were dried over Na2SO4, filtered and concentrated in vacuo. The crude product was purified by flash column chromatography, with a gradient from 10% to 100% EtOAc in heptane. The product contain fractions were combined and reduced in vacuo to yield the title compound as a yellow oil (7.0 g, 92% yield). 1H NMR (250 MHz, Chloroform-d) delta 3.85 (d, J=11.9 Hz, 2H), 3.53 (dd, J=9.8, 4.3 Hz, 1H), 3.41 (dd, J=9.8, 7.0 Hz, 1H), 3.00-2.86 (m, 1H), 2.85-2.57 (m, 3H), 2.57-2.36 (m, 1H), 1.40 (s, 9H), 0.84 (s, 9H), 0.00 (s, 6H). LCMS Method 1 [ELS]-Tr=0.92 min (ES+) (M+H+) 331.25.

As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (519 pag.)US2018/127370; (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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

3-Bromopropan-1-ol (20 ml, 20 mmol) was added dropwise to a solution of 1-methylpiperazine (29 ml, 26 mmol) in ethanol (200 ml). Potasium carbonate (83 gr, 60 mmol) was added and the mixture was refluxed for 20 hours. After cooling, the solid was filtered and the filtrate was evaporated. The residue was triturated with ether, filtrate and evaporated. The residue was distilled at about 60-70 C. under about 0.2 mm Hg to give 1-(3-hydroxypropyl)-4-methylpiperazine (17 g, 53%). 1H NMR Spectrum: (CDCl3) 1.72 (m, 2H); 2.3 (s, 3H); 2.2-2.8 (m, 8H); 2.6 (t, 2H); 3.8 (t, 2H); 5.3 (br s, 1H), 109-01-3

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

Reference£º
Patent; Hennequin, Laurent Francois Andre; US2003/199491; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: To a solution of piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester (10.6 g, 43 mmol) in 250 mL of dichloromethane was added (Boc)2O (19 g, 86 mmol) at 0 C. The reaction mixture stirred for 4 hours at room temperature, and then quenched with water and then extracted with dichloromethane. After the organic layer was dried over anhydrous Na2SO4, the filtrate was concentrated. The residue was purified by silica gel column chromatography to give Compound AH (yield 13.6 g, 92%).

129799-08-2, 129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; HOFFMANN-LA ROCHE INC.; Guo, Lei; Hu, Taishan; Kou, Buyu; Lin, Xianfeng; Shen, Hong; Shi, Houguang; Yan, Shixiang; Zhang, Weixing; Zhang, Zhisen; Zhou, Mingwei; Zhu, Wei; US2015/252057; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Example 75 N-{2- [3 -Fluoro-5- (4-isopropyl-piperazin- 1 -yl) -phenyl] -3 ,3 -dimethyl- 1 ,2,3 ,4- tetrahydro-quinoline-6-carbonyl}-methanesulfonamideA mixture of 2-(3-bromo-5-fiuoro-phenyl)-3,3-dimethyl-l,2,3,4-tetrahydro-quinoline-6- carboxylic acid methyl ester (0.41 g, 1.0 mmol), 1-isopropyl piperazine (0.64 g, 5.0 mmol), copper (I) iodidie (120 mg, 0.6 mmol), L-proline (69 mg, 0.6 mmol) and potassium hydroxide (33.6 mg, 0.6 mmol) in DMSO (2 mL) was stirred at 120 ¡ãC for 2 hours. Then treated with saturated ammonium chloride (20 mL), extracted with ether (100 mL). After removal of solvent, the residue was purified on flash silica gel chromatography (silica gel from QingDao, 200-300 mesh, glass column from Shanghai SD company)(40percent ethyl acetate/hexanes) to afford 2-[3-fiuoro-5-(4-isopropyl-piperazin-l-yl)-phenyl] -3,3- dimethyl-l,2,3,4-tetrahydro-quinoline-6-carboxylic acid ethyl ester (0.27 g, 60percent) as a white solid: LC/MS m/e calcd for C27H36FN3O2 (M+H)+: 454.6, observed: 454.3.

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; CHEN, Li; FENG, Lichun; HUANG, Mengwei; LIU, Yongfu; WU, Guolong; WU, Jim, Zhen; ZHOU, Mingwei; WO2011/128251; (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.244132-27-2,(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of 2-[4-(4-amino-phenylethynyl)-l-methyl-lH-pyrazol-3-yl]-4- chloro-phenol 4C (3.24 g, 10 mmol) in methylene chloride (250 mL) was added acid 3 (5.43 g, 12 mmol) and diisopropylcarbodiimide (2.3 mL, 15 mmol) at rt. The reaction was stirred at ambient temperature overnight. The solvent was removed under vacuum and the residue was purified on column to give 6.5 g of product in 86percent yield.

244132-27-2, 244132-27-2 (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 7128304, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; XTL BIOPHARMACEUTICALS LTD; WO2008/48589; (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.59702-31-7,1-Ethylpiperazine-2,3-dione,as a common compound, the synthetic route is as follows.,59702-31-7

Step A (4-Ethyl-2,3-dioxo-piperazin-1-yl) -acetic Acid To a solution of N-ethylpiperazin-2,3-dione (1.0 g, 7.0 mmol) in 10 mL of t-butanol over ice is added solid K2CO3 (1.1 g, 8.0 mmol). After stirring a few minutes t-butylbromoacetate (1.2 mL, 8.1 mmol) is introduced dropwise. The resultant mixture is stirred overnight at ambient temperature. The t-butanol is then azeotroped off with cyclohexane and the residue is partitioned between EtOAc and brine. The phases are separated and the organic phase is extracted 2*1M HCl, 2*saturated NaHCO3, and 2*brine; dried over Na2SO4; and concentrated to give the ester as a white solid (0.35 g, 1.4 mmol, 19%).

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

Reference£º
Patent; Gailunas, Andrea; Tucker, John A.; TenBrink, Ruth; Mickelson, John; US2003/109559; (2003); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of czs-2,6-dimethylpiperazine (1.00 g, 8.70 mmol) in CHC13 (20 mL) was added Boc anhydride (1.90 g, 8.70 mmol) drop-wise at 0 C, and the reaction mixture was stirred at room temperature for 16 h. The reaction mixture was diluted with DCM (30 mL) and washed with H20 (30 mL). The organic layer was separated, washed with brine (10 mL), dried over anhydrous Na2S04 and concentrated in vacuo to afford tert-butyl cz5-3,5-dimethylpiperazine-l- carboxylate (1.82 g crude) as an off-white solid. This compound was used as such for the next reaction without further purification. LC/MS (ESI) m/e [M+H]+/RT (min)/%: (0321) 215.00/2.52/83.4%. 1H NMR (400 MHz, DMSO-d6) delta 1.05 (d, J = 6.1 Hz, 6H), 1.20 (d, J = 6.7 Hz, 1H), 1.46 (s, 9H), 2.32-2.40 (m, 2H), 2.72-2.82 (m, 2H), 3.80-4.02 (m, 2H)., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference£º
Patent; NEUROPORE THERAPIES, INC.; WRASIDLO, Wolfgang; STOCKING, Emily, M.; HALL, Adrian; MACCOSS, Malcolm; (139 pag.)WO2017/20010; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 130D 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide To a solution of EXAMPLE 3J (90 mg), EXAMPLE 130C (64.2 mg), triethylamine (0.077 ml), N,N-dimethylpyridin-4-amine (38.5 mg) in a mixture of dichloromethane (5 ml) and N,N-dimethylformamide (0.5 ml) was added N1-((ethylimino)methylene)-N3,N3-dimethylpropane-1,3-diamine, hydrochloric acid (60.4 mg) and the mixture was stirred 18 hours. This was concentrated on high vacuum and the crude was purified by reverse phase chromatography with ammonium acetate buffer/acetonitrile. 1H NMR (500 MHz, pyridine-d5) delta 13.03 (s, 1H), 9.27 (d, 1H), 8.59 (d, 1H), 8.43 (d, 1H), 8.37 (dd, 1H), 8.11 (d, 1H), 7.65-7.67 (m, 2H), 7.44 (d, 2H), 7.07 (d, 2H), 6.88 (d, 1H), 6.76 (dd, 1H), 6.54 (d, 1H), 6.48 (m, 1H), 4.06 (m, 1H), 3.98 (d, 2H), 3.35 (t, 2H), 3.07 (m, 4H), 2.73-2.80 (m, 4H), 2.68-2.72 (m, 1H), 2.36 (q, 1H), 2.11-2.30 (m, 9H), 1.97 (m, 2H), 1.62-1.71 (m, 3H), 1.48-1.58 (m, 2H), 1.39 (t, 2H), 0.94 (s, 6H)., 1235865-77-6

The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBOTT LABORATORIES; US2010/305122; (2010); 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.

A mixture of 3-bromopropanol (20 ml), N-methylpiperazine (29 ml), potassium carbonate (83 g) and ethanol (200 ml) was stirred and heated to reflux for 20 hours. The mixture was cooled to ambient temperature and filtered. The filtrate was evaporated and the residue was triturated under diethyl ether. The resultant mixture was filtered and the filtrate was evaporated. The residue was purified by distillation at about 60-70C under about 0.2 mm Hg to give 1- (3-hydroxypropyl)-4-methylpiperazine (17 g); NMR Spectrum: (CDC13) 1.72 (m, 2H), 2.3 (s, 3H), 2.2-2. 8 (m, 8H), 2.6 (t, 2H), 3.8 (t, 2H), 5.3 (br s, 1H)., 109-01-3

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

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/4732; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics