Month: May 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

EXAMPLE-6 2-Cyano-1-(4-isopropyl-2-piperazinyl)-carbonyl Pyrrolidine Trifluoroacetate (Compound No.2). Step-1 To an aqueous (100 ml) sodium hydroxide (4.0 g, 100 mmol) solution of piperazine-2-carboxylic acid dihydrochloride (5 g, 24.63 mmol) is added a solution of di-tert-butyl dicarbonate (11.0 g, 50.45 mmol) in dioxan (50 ml) at 0 C. over a period of half an hour. The reaction mixture is stirred at 0 C. for 1 hr. followed by stirring at room temperature (25 C.) for another 2 hrs. Neutralized (pH 6-7) with aqueous 2N HCl, extracted with ethyl acetate. Organic layer washed with brine solution, dried (Na2SO4) and evaporated in vacuo to yield an oil which solidifies on cooling. (Yield 8.02 g, 98.76%)., 3022-15-9

As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference：
Patent; TORRENT PHARMACEUTICALS LTD.; US2004/106802; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55276-43-2, 1-Methanesulfonylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55276-43-2, A mixture of 2-biphenylylcyanamide (3.8 g), 1-methanesulphonylpiperazine (3.8 g) and ethanol (60 ml) was heated at 90-95 C. for 12 hours to give N-(2-biphenylyl)-4-methanesulphonylpiperazine-1-carboxamidine (m.p. 178-180 C.) which was recrystallized from ethanol.

55276-43-2 1-Methanesulfonylpiperazine 709161, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; The Boots Company; US5302720; (1994); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34334-28-6, 4-(4-Methylpiperazin-1-yl)benzonitrile is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 2-((4-chlorophenyl)thio)acetohydrazide 50(1.00 mmol), the suitably substituted nitrile (3.00 mmol), andK2CO3 (0.5 mmol) in n-BuOH (2 mL) was stirred for 16 h in a reusablesealed tube at 150 C, in an oil bath. The progress of the reactionwasmonitored by the disappearance of the hydrazide by TLCanalysis. The solvent was removed in vacuo and the residue obtainedwas purified by flash chromatography (hexanes/EtOAc 1:1).4.7. 5-(4-Chlorophenyl)-3-(((4-chlorophenyl)thio)methyl)-1H-1,2,4-triazole, 5White solid. M. p. 121e122 C. Yield: 51%. 1H-NMR (d, ppm):10.63 (bs, 1H, exc.), 7.93 (d, 2H, J 8.4 Hz), 7.42 (d, 2H, J 8.0 Hz),7.31e7.25 (m, 4H), 4.27 (s, 2H). 13C-NMR (d, ppm): 159.52, 156.95,136.28, 133.43, 132.72, 131.22, 129.41, 129.13, 128.54, 127.74, 127.49,30.34. HRMS (ESI) [M H] calculated for C15H11Cl2N3S: 335.0051,found: 335.0233., 34334-28-6

34334-28-6 4-(4-Methylpiperazin-1-yl)benzonitrile 763205, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; La Pietra, Valeria; Sartini, Stefania; Botta, Lorenzo; Antonelli, Alessandro; Ferrari, Silvia Martina; Fallahi, Poupak; Moriconi, Alessio; Coviello, Vito; Quattrini, Luca; Ke, Yi-Yu; Hsing-Pang, Hsieh; Da Settimo, Federico; Novellino, Ettore; La Motta, Concettina; Marinelli, Luciana; European Journal of Medicinal Chemistry; vol. 150; (2018); p. 491 – 505;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
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.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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
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.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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics