Heterocyclic Building Blocks-piperazine

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.,4318-42-7

Example 16 Preparation of 1-isopropyl-4-(6-nitropyridin-3-yl)piperazine A mixture of 5-bromo-2-nitropyridine (18.0 g, 88.7 mmol), N-isopropylpiperazine (17.1 g, 133 mmol) and potassium carbonate (36.9 g, 267 mol) in dimethylsulfoxide (200 mL) was stirred at 100¡ã C. for 16 h. After this time, the reaction was cooled to room temperature, poured into ice water (500 mL), stirred for 15 min, then extracted with ethyl acetate (2*500 mL). The combined organic layers were dried over sodium sulfate, filtered and the filtrate concentrated under reduced pressure. The resulting residue was dried under vacuum to a constant weight to afford 1-isopropyl-4-(6-nitropyridin-3-yl)piperazine as a yellow solid: 1H NMR (400 MHz, CDCl3). d 8.15 (d, J=9.2 Hz, 1H), 8.12 (d, J=2.8 Hz, 1H), 7.18 (dd, J=9.2, 2.8 Hz, 1H), 3.46 (t, J=4.8 Hz, 4H), 2.78-2.74 (m, 1H), 2.69 (t, J=5.2 Hz, 4H), 1.09 (d, J=10.8 Hz, 6H).

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Gilead Connecticut, Inc.; Blomgren, Peter A.; Currie, Kevin S.; Kropf, Jeffrey E.; Lee, Seung H.; Mitchell, Scott A.; Schmitt, Aaron C.; Xu, Jianjun; Zhao, Zhongdong; US2014/148430; (2014); A1;,
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74879-18-8,74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 25A (3S)-3-methyl-1-pyridin-2-ylpiperazine (S)-(+)-2-Methylpiperazine (0.50 g, 0.005 mol, Aldrich) and 2-bromopyridine (5 mL, 0.05 mol) were combined and heated at 120 C. for 14 hours. The reaction mixture was allowed to cool to 23 C. and partitioned between ethyl acetate and water. The layers were separated, and the water layer extracted twice with ethyl acetate. The aqueous phase was brought to pH~11 with a solution of saturated sodium bicarbonate and solid sodium carbonate. Sodium chloride was added, and the saturated aqueous solution was extracted with ethyl acetate (2*) and dichloromethane (2*). The combined organic extracts were dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure to afford 0.6 g (67% yield) of the title compound. 1H NMR (400 MHz, DMSO-d6) delta 1.02 (d, J=6.0 Hz, 3H), 2.27 (dd, J=10, 12 Hz, 1), 2.67 (m, 3H), 2.92 (m, 1H), 4.07 (m, 2H), 6.58 (dd, J=6, 8 Hz, 1H), 6.77 (d, J=8 Hz, 1H), 7.49 (m, 1H), 8.08 (m, 1H); MS (ESI) m/e 178 (M+H)+.

The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Cowart, Marlon D.; Patel, Meena V.; Kolasa, Teodozyi; Brioni, Jorge D.; Rohde, Jeffrey J.; Engstrom, Kenneth M.; Stewart, Andrew O.; Daanen, Jerome F.; Bhatia, Pramila A.; US2004/127504; (2004); A1;,
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20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 60 (100 mg, 0.213 mmol) was dissolved in DMSO. After adding N-cyclopropylpiperazine (134 mg, 1.06 mmol), The reaction was carried out at 120 C for 10 hours. The reaction was quenched by the addition of a small amount of water and extracted three times with dichloromethane. Washed three times with saturated brine, dried over anhydrous magnesium sulfate, filtered and evaporated. Column chromatography to give the title compound (yellow solid, 48mg), The yield was 39%.

20327-23-5, As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference£º
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Shen Jianhua; Xu Yechun; Huang Fubao; Liu Qiufeng; Wang Kai; (79 pag.)CN109651208; (2019); A;,
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196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a) 4-(5-Hydroxymethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl ester; To a solution of 179 mmol 30% aqueous hydrogen peroxide in 60 ml water was added 1 N aqueous sodium hydroxide solution until the pH was 9. The reaction mixture was then cooled to 100C and 163 mmol acrolein was added dropwise. Further amounts of 1 N aqueous sodium hydroxide solution were added during the addition in order to maintain the pH of the reaction mixture between pH 8 and 9. The mixture was stirred for 30 min at 0 0C and then 40.8 mmol thiocarbamoyl-piperazine-1-carboxylic acid tert- butyl ester (prepared from tert-butyl 1-piperazinecarboxylate, 1,1′- thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054) was added. To the resulting suspension was added 25 ml ethanol and the mixture was heated at 80 0C for 30 min. The resulting solution was diluted with ethyl acetate/tetrahydrofuran (1:1) and the mixture was washed twice with brine. The organic phase was dried over sodium sulphate and concentrated in vacuo to afford the title compound as a yellow oil (yield 99%). MS (m/e): 300.3 (M+H+, 100%)., 196811-66-2

196811-66-2 tert-Butyl 4-carbamothioylpiperazine-1-carboxylate 12093220, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; WO2006/72436; (2006); A1;,
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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.

Alternative preparation of 3-(4-methylpiperazin-1-yl)propyl{3-[3-(3,5-difluorophenyl)-6-oxo-6H-pyridazin-1-ylmethyl]phenyl}carbamate 600 mg (2.02 mmol) of bis(trichloromethyl) carbonate and 2.10 ml (15.1 mmol) of triethylamine is added successively to a solution, kept at 0 C., of 1.55 g (4.95 mmol) of 2-(3-aminobenzyl)-6-(3,5-difluorophenyl)-2H-pyridazin-3-one in 20 ml of dichloromethane. 850 mg (5.37 mmol) of 3-(N-methylpiperazine)propan-1-ol is then added, and the reaction mixture is stirred at room temperature for 18 hours. The reaction mixture is partitioned between 1 N NaOH and dichloromethane. The organic phase is dried over sodium sulfate and evaporated. The residue is chromatographed on a silica-gel column with dichloromethane/methanol: 3-(4-methylpiperazin-1-yl)propyl{3-[3-(3,5-difluorophenyl)-6-oxo-6H-pyridazin-1-ylmethyl]phenyl}carbamate as colourless crystals., 5317-33-9

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK PATENT GESELLSCHAFT MIT BESCHRAeNKTER HAFTUNG; US2011/136819; (2011); A1;,
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50606-32-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

8.3. 4-[(R)-2-tert-Butoxycarbonylamino-3-(diethoxy-phosphoryl)-propionyl]-piperazine-l- carboxylic acid butyl esterTo a solution of intermediate 8.2 (7.37 g) in CH2Cl2 (95 mL), THF (24 mL) and DIPEA (16.3 mL) were added HOBT (3.83 g) and EDCI-HCl (4.78 g), and the reaction mixture was stirred at RT for 10 min. Subsequently, piperazine- 1 -carboxylic acid butyl ester (5.31 g) was added and the mixture stirred at RT for 2.5 h. The reaction mixture was diluted with CH2Cl2, the org. phase washed with sat. aq. NaHCO3 and the aq. phase re-extracted with CH2Cl2. The combined org. phases were washed with brine, dried over Na2SO^ and concentrated to dryness. Purification by CC (EtOAc/MeOH 1 :0 to 9: 1) gave 7.66 g of the desired product. LC-MS: tR = 0.94 min; [M+H]+: 494.00.

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

Reference£º
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; LEHMANN, David; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/122504; (2010); A1;,
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75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 14;: 5-fluoro-2-[(3R)-3-methylpiperazin-l-yl]pyrimidine; HN,A solution of 2-chloro-5-fluoropyrimidine (239 mg, 1.80 mmol) and (R)-2-methylpiperazine (271 mg, 2.71mmol) in iPrOH (1 mL) and DIEA (617 uL) was heated in MW at 130¡ãC for 30 min. Solvent was removed under reduced pressure and the crude (600 mg) was purified by chromatography on silica using DCM/methanol (9/1) as eluent to afford The title compound as a white solid (416 mg, quantitative). TLC- DCM / MeOH(8/2); R/ 0.3. JH NMR (DMSO-d6) 5 8.14 (s, 2H), 4.48 (d, J = 13.2 Hz, 2H), 4.33 (bra,1H), 2.98-3.13 (m, 2H), 2.83 (m, 2H), 2.67 (t, J = 12.7 Hz, 1H), 1.20 (m, 3H)., 75336-86-6

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

Reference£º
Patent; Applied Research Systems ARS Holding N.V.; WO2006/10751; (2006); A1;,
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262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

262368-30-9, 17.6 g of N- (4-aminophenyl) -N, 4-dimethyl-1-piperazineacetamideAnd methyl N-acetyl-3- [methoxy (phenyl) methylene] -2-oxoindoline-6-carboxylate19 g was added to 75 mL of DMF 15 mL / methanol,Reflux reaction 1.5h or more.The reaction solution was added piperidine 9.4g, the reaction 1h, cooling,Filtration to 5 C.Nidanibu product 25.1g.According to the HPLC test, the amount of impurity compound in the nadinib was 0.03%.250 ml of nidadibugar methanol was recrystallized,The purity of purified nidadipine was 99.58%Impurity compounds were not detected.

As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference£º
Patent; Ruiyang Pharmaceutical Co., Ltd.; Hu Qingwen; Cong Chao; Wang Hongguang; Yu Zhibo; (9 pag.)CN106748961; (2017); A;,
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Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 9 In a 100 ml four-neck flask, 5.06 g (= 0.0505 mole) of racemic 2-methylpiperazine was placed, and 50.00 g of 1-butanol (water content 0.05 wtpercent) was added for dissolution. After cooling down to 0¡ãC, 10.91 g (= 0.0500 mole, 0.99 molar time) of di-tert-butyl dicarbonate was added dropwise with the liquid temperature kept in a range from 5 to 15¡ãC. Then, stirring was carried out at 5 to 10¡ãC for 2 hours. The reaction solution was analyzed, and as a result, the conversion of 2-methylpiperazine was 94.7percent, while the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 89.3percent (reaction yield 84.6percent).Example 10 An experiment was carried out as described for Example 9, except that the amount of di-tert-butyl dicarbonate used was changed to 11.97 g (= 0.0548 mole, 1.10 molar times). As a result, the conversion of 2-methylpiperazine was 100.0percent, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 81.5percent (reaction yield 81.5percent)., 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-39-4,(S)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 4; (8aS)-N-q,3-Dichlorophenyl)-l,3-dioxo-2-ralphaS,2R)-2- phenylcyclopropyllhexahydroimidazorLS-alpyrazine-TflHVcarboxamide (D3); Step 1 : 1-tert-Butyl 3-methyl (3S)-4-((r(lS.2R)-2-phenylcvclopropyllaminolcarbonvn-1.3- piperazinedicarboxylate (Dl); A solution of l-tert-buty 3-methyl (35)-l,3-piperazinedicarboxylate (AA3) in DCM (0.17 M) was added to a stirred solution of [(li?,25)-2-isocyanatocyclopropyl]benzene (1.0 eq.) in DCM (0.17 M) and the mixture was stirred at RT for 1 h. Solvents were evaporated under reduced pressure to give the title compound that was used as such in next step. MS (ES+) C2iH2gN3theta5 requires 403, found: 404 (M+H)+., 314741-39-4

314741-39-4 (S)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 1501855, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.; BRANCA, Danila; FERRIGNO, Federica; HERNANDO, Jose, Ignacio, Martin; JONES, Philip; KINZEL, Olaf; MALANCONA, Savina; MURAGLIA, Ester; PALUMBI, Maria, Cecilia; PESCATORE, Giovanna; SCARPELLI, Rita; WO2010/23480; (2010); A1;,
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