Month: March 2021

5308-25-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of 2 g (13 mmol) 2-chloro-5-nitro-pyridine and 0.76 g (6 mmol) N,N-diisopropylethylamine in 21 ml water and 4 ml DMF was heated to 80 C. During 2 min 1.73 g (15 mmol) N-ethylpiperazine was added and the mixture was kept for an additional hour at 80 C. The yellow precipitate was filtered off and washed three times with 4 ml water and dried for 16 h under vacuum to yield 2.48 g (83%) of the title compound as yellow crystals. (m/e): 237.1 (MH+; 100%).

As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference£º
Patent; Nettekoven, Matthias Heinrich; Roche, Olivier; Rodriguez-Sarmiento, Rosa Maria; US2006/122187; (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.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.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

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

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

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

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

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

5464-12-0,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.

EXAMPLE 22: 2-Chloro-6-(2-(4-methylpiperazin- 1 -yl)methoxy)pyridine31To a suspension of 2-(4-methylpiperazine-l-yl)ethanol (50mg, 0.347mmol) in dioxane (3ml) at 0¡ãC, KOlBu (50mg, 0.347mmol) was added and the reaction mixture was stirred for lOmin. Ice bath was removed and the reaction mixture was allowed to attain room temperature. The mixture was again cooled to 0¡ãC and 2, 6-Dichloropyrazine (200mg, 1.04mmol) was added. Reaction mixture was allowed to stir at RT for 24h after which it was concentrated and was purified by flash column chromatography over 230-400 silica gel using 5-8percent MeOH/DCM system to afford the desired product 31, 30mg (Yield:35 percent) as brown gummy liquid. The product was confirmed by 1HNMR (not clean but characteristic peaks were present); MS: 256, (M+l), LCMS -90percent.

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

Reference£º
Patent; ARRIEN PHARMAEUTICALS LLC; VANKAYALAPATI, Hariprasad; APPALANENI, Rajendra, P.; REDDY, Y., Venkata Krishna; WO2012/135631; (2012); 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.

75336-86-6, [1653] A solution of (R)-(-)-2-methylpiperazine (0.50 g, 0.005 mol, CAS 75336-86-6, Aldrich 39,716-4, 99percent) and 2-bromopyridine (5 mL, 0.05 mol) was heated to 120¡ã C. for 14 hours. The reaction mixture was cooled to 23¡ã C. and partitioned between a large volume of ethyl acetate and water. The layers were separated, and then additional water was added to the ethyl acetate solution. Drops of 1N Hydrochloric acid solution were added to the water/ethyl acetate mixture with vigorous mixing until all of the product was transferred to the aqueous phase. The layers were separated, and the combined aqueous phases concentrated under reduced pressure, and azeotroped with toluene/methanol (5.x.) to afford 1.29 g (>99percent yield) of 3-(R)-methyl-1-pyridin-2-yl-piperazine hydrobromide. 1H NMR (300 MHz, DMSO-d6) delta1.27 (d, J=6.6 Hz, 3H), 2.90 (dd, J=10.5, 14.1 Hz, 1H), 3.10 (m, 2H), 3.40 (m, 2H), 4.32 (m, 2H), 6.77 (dd, J=4.8, 6.9 Hz, 1H), 6.98 (d, J=8.1 Hz, 1H), 7.64 (m, 1H), 8.15 (m, 1H), 8.63 (br s, 1H), 8.92 (br s, 1H); MS (ESI) m/e 178 (M+H)+.

75336-86-6 (R)-2-Methylpiperazine 7330434, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Bhatia, Pramila A.; Daanen, Jerome F.; Hakeem, Ahmed A.; Kolasa, Teodozyj; Matulenko, Mark A.; Mortell, Kathleen H.; Patel, Meena V.; Stewart, Andrew O.; Wang, Xueqing; Xia, Zhiren; Zhang, Henry Q.; US2003/229094; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics