Heterocyclic Building Blocks-piperazine

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: In the nitrogen atmosphere of the glove box, 3.33 mg of ruthenium complex 1c was dissolved in 50 mL of tetrahydrofuran. After stirring, a catalyst 1c stock solution was formed. 1 ml of the above solution was added to a 125-mL Parr autoclave (0.067 mg, 0.0001 mmol). 1c), And added 9mL of tetrahydrofuran, Morpholine (8.712 g, 100 mmol). After the autoclave is sealed, it is taken out of the glove box. The carbon dioxide gas and hydrogen gas were each charged at 40 atm. The reaction system is heated to 120 C in an oil bath. The pressure rises to about 120 atm, After stirring for 181 hours, The reactor was then cooled to room temperature in a water bath. Slowly release the remaining gas in the fume hood, A pale yellow liquid was obtained. P-xylene (200 muL) was added to the mixture as an internal standard. The yield of N-formylmorpholine was determined by gas chromatography to be 94%.

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference：
Patent; Chinese Academy Of Sciences Shanghai Organic Chemistry Institute; Ding Kuiling; Qiu Jia; Yan Tao; Zhang Lei; Wang Zheng; (49 pag.)CN109553641; (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.149057-19-2,4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

54b. 4-Benzyl 1-terf-butyl 2-(methylcarbamoyl)piperazine-1,4- dicarboxylate4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (1.70 g, 4.70 mmol), DMF (20 ml_), diisopropylethylamine (2.50 mL, 14.1 mmol) and methylamine hydrochloride (0.350 g, 5.20 mmol) were mixed together at room temperature under argon for 10 minutes. 2-(7-aza-1 H- benzotriazole-1-yl)-1 ,1 ,3,3-tetramethyluronium hexafluorophosphate (HATU, 2.00 g, 5.20 mmol) was then added to the reaction mixture in one portion. The mixture was stirred at room temperature under argon for 18 hours. The reaction mixture was then poured into water (100 mL) and extracted with ethyl acetate (4 x 25 mL). The combined organic phases were washed with saturated ammonium chloride (3 x 15 mL), water (3 x 15 mL) and brine (70 mL). The combined organic phases were then dried over sodium sulfate, filtered and concentrated in vacuo. The product, obtained as a white foam (0.91 g, 2.4 mmol, 51%) was purified by column chromatography (gradient elution 20:80 ethyl acetate: hexanes to 100% ethyl acetate), Rf = 0.10 (50:50 ethyl acetate: hexanes); 1H-NMR (400 MHz, CDCI3) delta 7.39-7.33 (m, 5H), 5.17 (br s, 2H), 4.68-4.58 (m, 2H), 3.98-3.88 (m, 2H), 3.23-3.08 (m, 4H), 2.07 (s, 3H), 1.50 (S, 9H); Mass spectrum (ESI +ve) m/z 378.0 (MH+)

149057-19-2, 149057-19-2 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 2756778, apiperazines compound, is more and more widely used in various fields.

Reference：
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.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.,182618-86-6

The solvent was removed and the residue was taken up with methanol, Pd-C (10%) was added and stirred under hydrogen overnight at room temperature and then filtered through Celite and concentrated in vacuo. The crude product was purified by flash chromatography to afford 0.457 g product (60%).

As the paragraph descriping shows that 182618-86-6 is playing an increasingly important role.

Reference：
Article; Mou, Jianfeng; Park, Ann; Cai, Yu; Yuan, Junying; Yuan, Chengye; Bioorganic and Medicinal Chemistry Letters; vol. 25; 15; (2015); p. 3057 – 3061;,
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314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step D: tert-butyl (3)-4-[2-(3-cyano-4-fluorophenyl)-2-oxoethyl]-3-(hydroxymethyl)piperazine-1-carboxylate; 5-(Bromoacetyl)-2-fluorobenzonitrile (590 mg, 2.44 mmol) and (S)-4-N-BOC-2-hydroxymethyl-piperazine (527 mg, 2.44 mmol) were dissolved in THF (40 mL) at 0C thenTEA (247 mg, 2.44 mmol) was added. The reaction mixture was stirred at RT for 16 h, thenpoured into water and extracted with ethyl acetate. The organic layer was dried over Na2S04,filtered, and evaporated to dryness. The crude product was purified by MPLC through an 80g Redi-sep column using 0-100% EtOAc/hexane to yield the title compound., 314741-40-7

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

Reference：
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; WO2013/28474; (2013); A1;,
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548762-66-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(b) (2S,5R)-4-[5-(4-Bromo-3-trifluoromethoxy-phenylcarbamoyl)-pyridin-2-yl]-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester The product of the previous step (3.86 g, 10.2 mmol) (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (2.62 g, 12.2 mmol) and N,N-diisopropylethylamine (5.32 mL, 30.5) was dissolved in DMSO (12 mL). The reaction mixture heated at 120 C. for 3 h, diluted with EtOAc (100 mL), washed with water, and saturated NH4Cl, water, and brine. The reaction mixture was evaporated to about 40% volume and 3 M HCl in cyclopentyl methyl ether (4.24 mL, 12.7 mmol) was added slowly. Seeds from a previous run at smaller scale were added and the reaction mixture was stirred for 2 days and filtered to provide the HCl salt of the title intermediate (5.15 g, 83% yield). Analytical HPLC: Retention time=21.1 min.

The synthetic route of 548762-66-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Thalladi, Venkat R.; Nzerem, Jerry; Huang, Xiaojun; Zhang, Weijiang; US2013/295048; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

3-Iodo-4-fluoro-methyl nicotinic acid (225 mg, 0.8 mmol) was dissolvedin N, N- dimethylformamide (5 mL), was added N, N- diisopropylethylamine (180mu, 1.09 mmol) and 2- (7-BTA) -Nu, Nu, Nu ‘, Nu’- tetramethyluroniumhexafluorophosphate (610 mg, 1.6 mmol), stirred for 5 min add 3 -trifluoromethyl-4- (4-methyl-piperazinyl small ylmethyl) aniline (198 mg, 0.72mmol), the reaction mixture was stirred at room temperature 26 h. Aftercompletion of the reaction system was added water, extracted with ethyl acetatetwice. The combined organic layer was purified by column chromatography togive 4-fluoro-3-iodo -N- [4- (4- methyl – piperazin-1-ylmethyl)-3-trifluoromethyl – phenyl] – nicotinamide (white solid, 420 mg)., 694499-26-8

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference：
Patent; Shanghai Pharmaceuticals Holding Co.,Ltd .; WAN, HUIXIN; LI, CHUNLI; SHI, Chen; Liu, Haiyan; Li, Ping; XIA, Guangxin; HAN, Yanan; (52 pag.)CN103420977; (2016); B;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.197638-83-8,1-Boc-4-(4-Formylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: A solution of the pyridine (1.0 eq.) in dry. THF (0.1 M) was treated dropwise with s-BuLi solution (1.4 M in cyclohexane, 1 eq.) at 78 C and stirred at this temperature for 1 h. The reaction solution was then treated with a solution of the aldehyde or the isocyanate (2.5 eq.) in dry THF (1.2 M), and the reaction mixture was slowly warmed to rt overnight. After the addition of water and sat. amMonium chloride solution, the heterogeneous mixture was extracted three times with EtOAc. The combined organic layers were washed with sat. sodium chloride solution, dried over anhydrous magnesium sulfate, and the crude product was concentrated in vacuo. The product was isolated by means of flash chromatography on silica gel.

197638-83-8, The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Robke, Lucas; Rodrigues, Tiago; Schroeder, Peter; Foley, Daniel J.; Bernardes, Goncalo J.L.; Laraia, Luca; Waldmann, Herbert; Tetrahedron; vol. 74; 35; (2018); p. 4531 – 4537;,
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74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,74879-18-8

In a sealed tube, 7-fluoro-2-(2-methyl-[l,2,4]triazolo[l,5-a]pyrimidin-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one (Intermediate (VT1), 30 mg, 0.101 mmol), (S)-2-methylpiperazine (30.4 mg, 0.304 mmol, 3 eq.) and TEA (51.2 mg, 70.6 mu, 0.506 mmol, 5 eq.) were dissolved in DMSO (2 ml). The reaction mixture was heated at 120 C for 12 hours. The crude was filtered to afford the title product (29 mg, 77%) as a yellow solid. MS m/z 377.2 [M+H]+.

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

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; GILLESPIE, Robert Jack; HASANE, Ratni; SARIE, Jerome Charles; (89 pag.)WO2016/184832; (2016); A1;,
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373608-48-1, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 50 mL RBF was added tert-butyl 4-(3-aminopropyl)piperazine-1-carboxylate (1.105 g, 4.54 mmol), DCE (Volume: 10.32 ml), 5-methylpicolinaldehyde (0.5 g, 4.13 mmol) and STAB-H (1.575 g, 7.43 mmol). The reaction was stirred overnight then diluted with DCM and quenched with 2M NaOH. The organic layer was dried with Na2SO4, filtered and concentrated to a yellow oil which was purified via silica gel chromatography (DCM 2 minutes, 10% B(80:20:3, DCM:MeOH:NH4OH) 5 minutes and 50% B 9 minutes) to afford tert-butyl 4-(3-(((5-methylpyridin-2-yl)methyl)amino)propyl)piperazine-1-carboxylate (0.75 g, 2.152 mmol, 52 % yield). 1H NMR (400 MHz, CDCl3): delta = 8.36 (d, J= 2.0 Hz, 1H), 7.44 (dd, J= 7.9, 2.2 Hz, 1H), 7.18 (d, J= 7.9 Hz, 1H), 3.87 (s, 2H), 3.42 (t, J= 5.1 Hz, 4H), 2.73 (t, J= 6.8 Hz, 2H), 2.42 (t, J= 7.1 Hz, 2H), 2.38 (t, J= 5.0 Hz, 4H), 2.31 (s, 3H), 1.75 (pent, J= 6.9 Hz, 2H), 1.45 (s, 9H);

373608-48-1, The synthetic route of 373608-48-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; WILSON, Robert James; NGUYEN, Huy Hoang; KIM, Michelle Bora; WILSON, Lawrence; MILLER, Eric James; TAHIROVIC, Yesim Altas; TRUAX, Valarie; KAISER, Thomas; (311 pag.)WO2018/156595; (2018); A1;,
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70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(E)-(3-(3-(2-(2-Pyridyl))vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole was added to a round bottom flask. 6-yl) thio)propionic acid (50 mg) followed by N,N-dimethylformamide (5 ml), 4-((4-methylpiperazin-1-yl)methyl)aniline (28 mg ),2-(7-oxidized benzotriazole)-N,N,N’,N’-tetramethylureaFluorophosphate (70 mg) and triethylamine (0.05 ml).The reaction system was stirred at room temperature for 14 hours under argon atmosphere.After the reaction is over,The system was evaporated to dryness under reduced pressure.The resultant was diluted with water and extracted with ethyl acetate.Organic phase with water,After washing with saturated brine, it was dried over anhydrous sodium sulfate.The organic phase is filtered,After evaporation under reduced pressure, the crude product was dissolved in anhydrous dichloromethane (5ML),Trifluoroacetic acid (1 mL) was added.The reaction system was stirred at room temperature for 14 hours under argon atmosphere.After the reaction,The system is evaporated to dryness under reduced pressure.The resultant was diluted with water and neutralized to pH > 10 with a saturated sodium hydrogen carbonate solution.The aqueous phase was extracted with ethyl acetate.Organic phase with water,After washing with saturated brine, it was dried over anhydrous sodium sulfate.The organic phase is filtered,After evaporation under reduced pressure, a crude product was obtained.The crude product was purified by column chromatography on silica gel to yield purified compound 134.

70261-82-4, As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference：
Patent; Chinese Academy Of Sciences Hefei Matter Sciences Institute; Liu Jing; Liu Qingsong; Liu Xuesong; Wang Beilei; Jiang Zongru; Yu Kailin; Chen Cheng; Zou Fengming; Liu Qingwang; Liu Xiaochuan; Wang Wei; Wang Wenliang; Hu Chen; Wang Wenchao; Wang Junjie; Wang Li; (82 pag.)CN109942544; (2019); A;,
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Piperazines – an overview | ScienceDirect Topics