Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 5 A reaction was carried out as described for Example 1, except that the solvent was changed from 44.7 g of 1-butanol to a mixed solvent consisting of 5.3 g of water and 40 g of 1-butanol (water content 10.6 wt%). After stirring at 0 to 5C for 2 hours, the reaction solution was analyzed. As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 82.1% (based on the amount of 2-methylpiperazine). Comparative Example 1 A reaction was carried out as described for Example 1, except that the solvent was changed from 44 g of 1-butanol to a mixed solvent consisting of 9 g of water and 35 g of 1-butanol (water content 20.5 wt%). After stirring at 0 to 5C for 2 hours, the reaction solution was analyzed. As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 59.6% (based on the amount of 2-methylpiperazine). Comparative Example 2 A reaction was carried out as described for Example 4, except that the solvent was changed from 44 g of 1-butanol to a mixed solvent consisting of 18 g of water and 27 g of 1-butanol (water content 40.0 wt%). After stirring at 0C for 2 hours, the reaction solution was analyzed. As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 51.6% (based on the amount of 2-methylpiperazine). Comparative Example 3 A reaction was carried out as described for Example 1, except that the solvent was changed from 44 g of 1-butanol to a mixed solvent consisting of 22 g of water and 22 g of 1-butanol (water content 50 wt%). After stirring at 0C for 2 hours, the reaction solution was analyzed. As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 33.6% (based on the amount of 2-methylpiperazine)., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
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103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,103-76-4

Step: 3A-lSynthesis of 2-[4-(4-Nitro-phenyI)-piperazin-l-yl]-ethanol. Procedure:K2C03 (3.912g, 0.02834mol) followed by 1 -Fluoro-4-nitro-benzene (2g, 0.01417mol) was added to a solution of 2-Piperazin-l-yl-ethanol (5.21ml, 0.0425 lmol) in DMF (10ml) and the reaction flask was maintained at 80C for 5hrs. The reaction was monitored by the TLC (10% MeOH: CHC13). The resultant was quenched with ice to afford 3g (86% yield) of 2-[4-(4-Nitro-phenyl)-piperazin-l-yl]-ethanol as a yellow solid.

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AURIGENE DISCOVERY TECHNOLOGIES LIMITED; SENGUPTA, Saumitra; RAJAGOPALAN, Srinivasan; BELAVAGI, Ningaraddi; RAMACHANDRA, Muralidhara; WO2012/59932; (2012); A1;,
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120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of tert-butyl piperazine-1-carboxylate (1 g, 5.37 mmol, 1.00 equiv), 6-chloropyridine-3-carbonitrile (690 mg, 4.98 mmol, 1.00 equiv), potassium carbonate (1.4 g, 10.13 mmol, 2.00 equiv), NMP (20 mL) was stirred for 1 h at 80 C. The resulting solution was quenched by 100 ml of water and extracted with 2¡Á100 mL of EtOAc and the organic layers combined and concentrated under vacuum to afforded 1.2 g (78%) of the title compound as yellow oil. LCMS (ESI, m/z): 303.15 [M+H]+, 120737-78-2

As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Patent; Ribon Therapeutics Inc.; Vasbinder, Melissa Marie; Schenkel, Laurie B.; Swinger, Kerren Kalai; Kuntz, Kevin Wayne; (410 pag.)US2019/330194; (2019); A1;,
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4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A: r5-(4-lsopropyl-piperazin-1 -yl)-2-(4-methylsulfanyl-phenoxy)- benzyli-methyl-carbamic acid tert-butyl ester.; A mixture of [5-bromo-2-(4- methylsulfanyl-phenoxy)-benzyl]-methyl-carbamic acid tert-butyl ester (300 mg, 0.684 mmol) {prepared in an analogous fashion to Example 1 , Steps A-C}, isopropyl piperazine (132 mg, 1.02 mmol), XPHOS (39 mg, 0.082 mmol), Pd2(dba)3 (62.6 mg, 0.0684 mmol), and t-BuONa (98.0 mg, 1.02 mmol) in toluene was heated in a sealed tube overnight at 120 0C. After cooling to rt, the mixture was filtered through diatomaceous earth and the filtrate was concentrated. Purification by FCC gave the desired product (180 mg, 54percent). MS (ESI): mass calcd. for C27H39N3O3S, 485.27; m/z found, 486.4 [M+H]+. 1H NMR (CDCI3): 7.22 (d, J = 8.5, 2H), 6.86-6.83 (m, 1 H), 6.83-6.80 (m, 4H), 4.42- 4.35 (m, 2H), 3.19-3.16 (m, 4H), 2.87-2.83 (m, 2H), 2.80-2.75 (m, 1 H), 2.75- 2.71 (m, 1 H), 2.71-2.67 (m, 4H), 2.44 (s, 3H), 1.48-1.40 (m, 9H), 1.10 (d, J = 6.5, 6H).

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/2820; (2008); A2;,
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122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: General procedure for the synthesis of 15b-15u. To a solution ofcompound 13a (0.41 g, 1.06 mmol) in 2-butanol (5 mL), 1-(2-(dimethylamino)ethyl)-1H-pyrazol-4-amine (0.196 g, 1.27 mmol)and trifluoroacetic acid (94 mL) were added in a sealed tube. Thereactionwas heated at 95 C for 18 h. The reaction mixturewas thenallowed to cool to room temperature. The mixture was transferredto a round-bottom flask and then the solvent was removed underreduced pressure. The residue was dissolved in DCM (2.0 mL) andTFA (2.0 mL), and the resulting mixture was stirred for 5 h at roomtemperature. The solvent was removed under reduced pressure,and the residue was neutralized with saturated NaHCO3 aqueoussolution. The water layer was extracted with DCM. The organiclayer was combined and washed with brine, dried over Na2SO4,filtered, concentrated, and purified by silica gel chromatography toafford 15a as a yellow solid (0.264 g, 65% for two steps).

122833-04-9, The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Yu, Lei; Huang, Minhao; Xu, Tianfeng; Tong, Linjiang; Yan, Xiao-e; Zhang, Zhang; Xu, Yong; Yun, Caihong; Xie, Hua; Ding, Ke; Lu, Xiaoyun; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 1107 – 1117;,
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112257-24-6, 1-Boc-3-Carbamoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (300mg, 0.64mmol), the compound 3-carbamoylpiperazine-1-carboxylate (153mg, 0.64mmol), 1- ethyl-3- (3-dimethylaminopropyl Aminopropyl)carbodiimide hydrochloride (250mg, 1.3mmol) and N- hydroxy-7-aza-benzotriazole (174mg, 1.3mmol) wasdissolved in methylene Methane (25mL), and the conditions under 0 C, to this solution was added dropwiseN, N- diisopropylethylamine (0.33mL, 1.93mmol), stirred at room temperature 5 H, add water (10mL ¡Á 3),dried over anhydrous Na 2 SO 4 organic phase was dried, the solvent was removed concentrate was subjected tocolumn chromatography (eluent: Petroleumether / EtOAc (v / v) = 2/3), to give 220mg white solid, yield: 50%., 112257-24-6

As the paragraph descriping shows that 112257-24-6 is playing an increasingly important role.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, To a stirred suspension of 4-(bromomethyl)-6-(trifluoromethyl)pyridin-2-amine hydrobromide (2.10 g, 6.25 mmol) in acetonitrile (13 mL) was added potassium carbonate and cyclopropyl(piperazin-1-yl)methanone (1.06 g, 6.88 mmol). The mixture was stirred atr.t. for 14 h. Water was added and the mixture was extracted with ethyl acetate. The organic phase waswashed with half-saturated sodium chloride solution, dried (sodium sulfate) and the solvent was removed in vacuum. Ssilicage chromatography gave 2.00 g (98 % yield) of the title compound.LC-MS (Method 2): R = 0.94 mm; MS (ESipos): m/z = 329 [M+H]

59878-57-8 1-(Cyclopropylcarbonyl)piperazine 2064235, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; SCHULZE, Volker; HEINRICH, Tobias; PRINZ, Florian; LEFRANC, Julien; SCHROeDER, Jens; MENGEL, Anne; BONE, Wilhelm; BALINT, Joszef; WENGNER, Antje; EIS, Knut; IRLBACHER, Horst; KOPPITZ, Marcus; BOeMER, Ulf; BADER, Benjamin; BRIEM, Hans; LIENAU, Philip; CHRIST, Clara; STOeCKIGT, Detlef; HILLIG, Roman; (1256 pag.)WO2017/102091; (2017); 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-l-yl)ethyl 4-nitrophenyl carbonate To a stirred solution of l-(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, 37percent solution in water) The reaction mixture was cautiously heated at 100 0C for 2 hours and 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 0C, 2-(4-methylpiperazin-l-yl)ethanol (51 g, 44percent) as a colourless liquid. Analytical LCMS: (System B, Rtau = 0.70 min), ES+: 145.1 (100percent) [MH]+., 103-76-4

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

Reference£º
Patent; BIOVITRUM AB (publ); WO2009/71677; (2009); 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.

Preparation of l-methyl-4-r2-(4-{l-r3-(trifluoromethyl)ri,2,41triazolor4,3- blpyridazin-6-yllpiperidin-4-yl}phenoxy)ethyllpiperazin-2-oneDIPEA (15.27 niL, 87.69 mmol) was added to 2-(4-{l-[3-(trifluoromethyl)[l,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl}phenoxy)ethyl methanesulfonate (14.19 g, 29.23 mmol) and 1 -methylpiperazin-2-one (CAS 59702-07-7, 3.67 g, 32.15 mmol) in DMA (70 mL). The resulting solution was stirred at 1100C for 1 hour. The reaction mixture was cooled to room temperature, absorbed onto silica, evaporated to dryness and then purified by flash silica chromatography, elution gradient 0 to 3percent MeOH in DCM. Pure fractions were evaporated and the resulting gum was scratched with ether until solid. The solid was stirred in ether (100 mL) for 4 hours then collected by filtration and dried to give l-methyl-4-[2-(4-{l-[3- (trifTuoromethyl)[ 1 ,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4- yl}phenoxy)ethyl]piperazin-2-one (10.08 g, 68.5percent) as a solid.IH NMR (399.9 MHz, CDC13) delta 1.76 (2H, m), 2.00 (2H, m), 2.75 – 2.87 (5H, m), 2.95 (3H, s), 3.11 (2H, m), 3.28 (2H, s), 3.34 (2H, t), 4.09 (2H, t), 4.37 (2H, m), 6.86 (2H, d), 7.11 – 7.14 (3H, m), 7.92 (IH, d); m/z = 504 [M+H]+., 59702-07-7

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BRADBURY, Robert, Hugh; RABOW, Alfred, Arthur; WO2010/131022; (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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

109384-27-2, HATU (0.138 g, 0.363 mmol) was added to a mixture of 3-chloro-6-(3- furanyl)-8-(trifluoromethyl)imidazo[1 ,2-a]pyridine-2-carboxylic acid (0.1 00 g, 0.302 mmol), 1 -methyl-2-piperazinone hydrochloride (0.045 g, 0.302 mmol) and DIPEA (0.1 1 mL, 0.605 mmol) in DMF (1.5 mL). The mixture was stirred at room temperature overnight, The reaction mixture was diluted with ethyl acetate and washed with water. The organic layer was dried over sodium sulfate and the solvent was evaporated. The residue was purified by reverse phase HPLC (acetonitrile:water with 0.1 % formic acid) to afford 0.055 g of the title compound as a white solid. 1H NMR (400 MHz, DMSO-G(6) delta ppm 8.83 (d, J=6.96 Hz, 1 H) 8.58 (s, 1 H) 8.23 (s, 1 H ) 7.85 (s, 1 H) 7.34 (s, 1 H ) 4.46 (s, 1 H) 4.23 (s, 1 H) 4.05 (br. s., 1 H) 3.93 (br. s., 1 H ) 3.43 (m, 2 H) 2.91 (s, 3 H). ES-LCMS m/z: 426 (M+).

As the paragraph descriping shows that 109384-27-2 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; PEAT, Andrew, James; PRICE, Daniel, J.; SHOTWELL, John, Brad; TAI, Vincent; ZHANG, Huichang; WO2011/41713; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics