Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

Compound 63 (100 mg, 0.228 mmol) was dissolved in ultra dry THF. After adding N-cyclopropylpiperazine (144 mg, 1.14 mmol), Stir overnight at room temperature. 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, 37 mg), yield 31%., 20327-23-5

20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

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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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

278788-66-2, 2,6-difluoro-3-(oxiran-2-yl)benzonitrile (3.70 g, 20.4 mmol) and (R)-tert-butyl 3-(hydroxymethyl)piperazine-1-carboxylate (6.63 g, 30.6 mmol) were dissolved in ethanol (36.0 mL) then placed in 3-20mL sealed tubes andmicrowaved at 140C for 1 h. The solvents were evaporated and the combined residue was purified by chromatographythrough a 120g ISCO Redi-sep column with 50% to 100% ethyl acetate/hexane solvent system to yield thetitle compound LC-MS (IE, m/z): 398 [M + 1]+.

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Merck Sharp & Dohme Corp.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
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59878-57-8,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.

General procedure: Compound 6 (1.0 equiv) with catalytic equivalent KI was dissolved in freshly distilled DMF in an oven-dried round bottom flask. Different aliphatic amines (3.0 equiv) was added dropwise. The reaction mixture was stirred at room temperature for about 4h. After the reaction monitored by TLC was over, water was added to the reaction mixture under stirring, and the suspended mixture was filtered. The crude residue was purified by column chromatography on silica gel to obtain the final products.

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

Reference£º
Article; Chen, Lijuan; Chen, Yong; Deng, Dexin; Liu, Kongjun; Pei, Heying; Tang, Minghai; Xue, Linlin; Yang, Tao; Yang, Zhuang; Ye, Haoyu; Zheng, Shoujun; European Journal of Medicinal Chemistry; vol. 197; (2020);,
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181955-79-3, 1,4-Di-Boc-piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a dry flask were added 1, 4-di (tert-butoxycarbonyl) piperazine-2-carboxylic acid (14 g, 42.37 mmol) , potassium carbonate (11.7 g, 84.7 mmol) , acetone (200 mL) , iodomethane (5.3 mL, 85 mmol) in turn, the mixture was stirred at rt for 12 hours. The mixture was filtered, the filtrate was concentrated in vacuo and to the residue was added (200 mL) and water (200 mL) , the mixture was separated into layers, the organic layer was washed with saturated aqueous NaCl and dried over anhydrous sodium sulfate, then concentrated in vacuo to get the title compound as a white solid (13.55 g, 93%) . MS (ESI, pos. ion) m/z: 367.2 [M+Na] +.

181955-79-3, As the paragraph descriping shows that 181955-79-3 is playing an increasingly important role.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; LIU, Xinchang; REN, Qingyun; YAN, Guanghua; GOLDMANN, Siegfried; ZHANG, Yingjun; (253 pag.)WO2019/76310; (2019); A1;,
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5625-67-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

To a solution of piperazinone (10.0 g, 100 mmol), Triethylamine (20.2 g, 200mmol), and DMAP (50 mg) in CHaCIa (250 ml) in an ice water bath was added(Boc)2O (22.9 g, 105 mmol) slowly. The mixture was stirred in the ice-water bath for 1h and at RT for 4.5 h. The mixture was diluted with CH2CI2 (250 ml), washed withwater (200 ml), 5% citric acid (200 ml), 1N HCI (200 ml), saturated sodiumbicarbonate (20 ml) and brine. The organic layer was dried (MgSO4) andconcentrated to give the product (18.0 g, 90%). MS m/e 201 (M+H)”1″

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference£º
Patent; SCHERING CORPORATION; WO2006/14944; (2006); A1;,
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2762-32-5, Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

54a. 4-((Benzyloxy)carbonyl)-1 -(tert-butoxycarbonyl)piperazine-2- carboxylic acidThe tile compound was prepared according to the procedure of [Kempf, D. J.; Norbeck, D. W.; Sham, H. L U.S. Patent 5,455,351 , Oct 3, 1995]. Piperazine-2-carboxylic acid (10.0 g, 77.0 mmol) was dissolved in a 1 :1 solution of 1 ,4-dioxane:water (100 mL) at room temperature with vigorous stirring. The clear solution was adjusted to pH 11 by the addition of an aqueous solution of sodium hydroxide (80 mL of a 1Lambda/ solution). The pH was monitored in situ with a pH meter throughout the reaction. The reaction flask was fitted with an addition funnel that contained a solution of Lambda/-alpha- (benzyloxycarbonyloxy) succinamide (13.6 g, 55 mmol) in 1 ,4-dioxane (50 mL). The Lambda/-alpha-(benzyloxycarbonyloxy) succinamide solution was added over 45 minutes at room temperature and the pH was kept above 10 by the periodic addition of 1 Lambda/ sodium hydroxide. The pH of the solution was adjusted to 9.5 and 2-(teAf-butoxycarbonyloxyimino)-2-phenylacetonitrile (13.4 g, 55 mmol) was added as a solution in 1 ,4-dioxane (50 mL) over 10 minutes. The pH was maintained at 9.5 and the solution was stirred at room temperature for 17 hours. The solution was then acidified to pH 2 and the aqueous solution was washed with diethyl ether (3 x 150 mL). The aqueous solution was cooled to O0C and acidified by adding of concentrated hydrochloric acid. The acidic solution was extracted with ethyl acetate (5 x 150 mL). The combined organic phases were dried over sodium sulfate, filtered and concentrated in vacuo. The residue was triturated with a 1 :1 solution of dichloromethane: hexanes (150 mL) and the solvent was removed in vacuo to provide the product as a viscous yellow oil (15.7 g, 43 mmol, 80%). Rf = 0.60 (66:34 dichloromethane: ethyl acetate + 0.1% (v/v acetic acid); 1H-NMR (400 MHz, DMSO) delta 13.0 (br s, 1 H), 7.37-7.36 (m, 5H), 5.05 (s, 2H), 4.54-4.33 (m, 2H), 3.90-3.66 (m, 2H), 3.07-2.81 (m, 4H), 1.38 (s, 9H); Mass spectrum (ESI +ve) m/z 365.1 (MH+).

2762-32-5, The synthetic route of 2762-32-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIKAM PHARMACEUTICALS, INC.; GARVEY, David, S.; LAROSA, Gregory, J.; GREENWOOD, Jeremy, Robert; BREWER, Mark, L.; QUACH, Tan; COTE, Jamie, B.; BERMAN, Judd; WO2010/147653; (2010); 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.,5317-33-9

g) is thereby obtained in the form of cream-coloured crystals, m.p. 240 C. N-[3-(4-Methyl-1-piperazinyl)propoxy]phthalimide may be obtained in the following manner: a solution of 1-(3-hydroxypropyl)-4-methylpiperazine (8.4 g), N-hydroxyphthalimide (8.2 g) and triphenylphosphine (13.1 g) in tetrahydrofuran (120 cc) is cooled to a temperature in the region of 0 C. and ethyl azodicarboxylate (10.1 g) is added in the course of 30 minutes. The solution obtained is stirred at a temperature in the region of 20 C. for 18 hours and is then concentrated to dryness under reduced pressure (20 mm Hg; 2.7 kPa) at a temperature in the region of 60 C. The crude oil obtained is chromatographed on a column 5 cm in diameter containing silica (0.063-0.2 mm) (400 g). The column is eluted with mixtures of ethyl acetate and methanol, collecting 500-cc fractions. The first 5 fractions originating from elution with pure ethyl acetate and the next 5 fractions originating from elution with a mixture of ethyl acetate and methanol (70:30 by volume) are discarded. The next fraction originating from elution with a mixture of ethyl acetate and methanol (70:30 by volume), the next 5 fractions originating from elution with a mixture of ethyl acetate and methanol (50:50 by volume) and the next 2 fractions originating from elution with pure methanol are combined and concentrated to dryness under reduced pressure (20 mm Hg; 2.7 kPa) at a temperature in the region of 60 C. N-[3-(4-Methyl-1-piperazinyl)propoxy]phthalimide (11.4 g) is thereby obtained in the form of a red oil (Rf=0.2; thin-layer chromatography on silica, eluent: ethyl acetate/methanol, 50:50 by volume).

As the paragraph descriping shows that 5317-33-9 is playing an increasingly important role.

Reference£º
Patent; Rhone-Poulenc Sante; US5086051; (1992); A;,
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216144-45-5, 4-(4-Methylpiperazin-1-yl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation F; (3-chloro-4-(4-methylpiperazin-1-yl)phenyl)methanamine; Step F (1); To a solution of (4-(4-methylpiperazin-1-yl)phenyl)methanamine (204 mg, 1.0 mmol, Aldrich) in THF (2.0 mL) was added (Boc)2O (327 mg, 1.5 mmol) and NaOH/H2O (1.0 mL, 1 N). The mixture was stirred at rt for 1 h. EtOAc (100 mL) was added and the resulting solution was washed with H2O (2¡Á100 mL). The organic layer was dried and concentrated to give 250 mg (yield 82%) of tert-butyl 4-(4-methylpiperazin-1-yl)benzylcarbamate. LC-MS (M+H)+=306.35 1H-NMR(500 MHz, CD3OD) delta 7.18 (d, J=8.55 Hz, 2H), 6.94 (d, J=8.54 Hz, 2H), 4.15 (s, 2H), 3.16-3.22 (m, 4H), 2.60-2.66 (m, 4H), 2.36 (s, 3H), 1.46 (s, 9H).

216144-45-5, The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Bristol-Myers Squibb Company; US2007/49589; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,74879-18-8

Step l; 3-(5)-Methyl-l-(5-trifluoromethyl-pyridin-2-yl)-piperazine:; 2-Bromo-5-trifluoromethyl-pyridine (1.06 g, 4.69 mmol), (5)-2-methylpiperazine (1.03 g, 10.28 mmol) and triethylamine (1.5 mL, 10.76 mmol) were stirred in toluene (10 mL) at 110 0C for 26 h. The reaction was cooled to room temperature, diluted with ethyl acetate (150 mL) and washed with water and brine. The organic layer was dried (MgSC>4), filtered and concentrated. The crude mixture was purified by automated silica gel flash column chromatography (gradient eluent 0-20% MeOH/dichloromethane) to afford 3-(S)-methyl-l-(5-trifluoromethyI-pyridin-2-yl)- piperazine (926 mg, 81 %) as a yellow solid. 1H NMR (400 MHz, CDCl3) delta 8.38 (s, IH), 7.62 (dd, IH), 7.63 (d, IH), 4.29-4.20 (m, 2H), 3.16-3.12 (m, IH), 3.02-2.85 (m, 3H), 2.64-2.52 (m, 2H), 1.18 (d, 3H).

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference£º
Patent; KALYSPSYS, INC.; NOBLE, Stewart A.; OSHIRO, Guy; MALECHA, James W.; ZHAO, Cunxiang; ROBINSON, Carmen K. M.; DURON, Sergio G.; SERTIC, Michael; LINDSTROM, Andrew; SHIAU, Andrew; BAYNE, Christopher; KAHRAMAN, Mehmet; LOU, Boliang; GOVEK, Steven; WO2006/55187; (2006); A1;,
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77279-24-4,77279-24-4, tert-Butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Into a 50-mL round-bottom flask, was placed a solution of tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate (2.31 g, 10.03 mmol, 1.00 equiv) in dichloromethane (20 mL) and a solution of thionyl chloride (1.5 mL, 2.00 equiv) in dichloromethane (3 mL) was added dropwise at 0 C. The resulting solution was stirred overnight at 25 C. The resulting mixture was concentrated under vacuum. The resulting solution was diluted with 10 mL of water. The resulting solution was extracted with 2*25 mL of ethyl acetate and the organic layers combined. The resulting mixture was washed with 2*15 mL of sodium bicarbonate aq. and 2*10 mL of brine. The mixture was dried over anhydrous sodium sulfate and concentrated under vacuum. The residue was applied onto a silica gel column and eluted with ethyl acetate/petroleum ether (1:5). This resulted in 1.16 g (46%) of tert-butyl 4-(2-chloroethyl)piperazine-1-carboxylate as a off-white solid.

The synthetic route of 77279-24-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ardelyx, Inc.; Lewis, Jason G.; Jacobs, Jeffrey W.; Reich, Nicholas; Leadbetter, Michael R.; Bell, Noah; Chang, Han-Ting; Chen, Tao; Navre, Marc; Charmot, Dominique; Carreras, Christopher; Labonte, Eric; (323 pag.)US9301951; (2016); B2;,
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