Month: November 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.639068-43-2,tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,639068-43-2

tert-Butyl 3,5-dimethylpiperazin-1-carboxylate (200.0 mg, 0.93 mmol) and 37percent formaldehyde (440.0 muL, 5.56 mmol) were dissolved in MeOH (5.0 mL), and NaBH4 (172.6 mg, 5.56 mmol) was slowly added thereto and stirred at room temperature for 12 hours. Brine was poured into the reaction mixture, and it was extracted with DCM (30.0 mL). The organic layer was dried over anhydrous Na2SO4, filtered and then distilled under reduced pressure. The residue was purified column chromatography (DCM:MeOH=95:5) on silica to obtain yellow liquid compound of tert-butyl 3,4,5-trimethylpiperazin-1-carboxylate (57.0 mg, 27percent).

639068-43-2 tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 22219990, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; C&C RESEARCH LABORATORIES; Ho, Pil Su; Yoon, Dong Oh; Han, Sun Young; Lee, Won Il; Kim, Jung Sook; Park, Woul Seong; Ahn, Sung Oh; Kim, Hye Jung; US2014/315888; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55121-99-8, A solution of 4-(4-methylpiperazine-1-carbonyl)aniline (1.03g, 4.56 mmol) in THF (50 mL) was cooled to 0C and LiAlH41 M in THF (14 mL, 14 mmol) was added dropwise. The mixture was let to warm to room temperature, and then refluxed for 3 h. After cooling to 0C Na2SO4.10H2O was added and the solution was filtered off. The solution was concentrated and purified by silica flash chromatography with 0 to 5% MeOH in DCM to give 4-[(4- methylpiperazin-1-yl)methyl]aniline (500 mg, 53% yield). MS found for C12H19N3 as (M+H)+ 206.3.

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PHARMACYCLICS LLC.; ATALLAH, Gordana, Babic; CHEN, Wei; JIA, Zhaozhong, J.; POZZAN, Alfonso; RAVEGLIA, Lucal, Francesco; ZANALETTI, Riccardo; (815 pag.)WO2016/196776; (2016); A2;,
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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, 1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Triethylamine (3.83 mL) and di-tert-butoxydicarbonate (6.32 mL) were added at room temperature to piperazin-2-one (2.5 g) in a mixture of tetrahydrofuran (50 mL) and methanol (50 mL), followed by stirring for 4 hours. The reaction solvent was evaporated under reduced pressure. The residue was partitioned between water and ethyl acetate. The organic layer was sequentially washed with water and saturated brine. The aqueous layers obtained through washing were combined, and the combined layer was extracted with ethyl acetate. The organic layers were combined, followed by drying over magnesium sulfate anhydrate. After a filtration step, the solvent was evaporated under reduced pressure. Subsequently, ethyl acetate-hexane was added to the residue, followed by drying to solid, to thereby give 3-oxopiperazine-1-carboxylic acid tert-butyl ester (3.6 g, 72%). 1H-NMR(400MHz,CDCl3)delta:1.48(9H,s), 3.37-3.40(2H,m), 3.62-3.65(2H,m), 4.01(2H,s), 6.32(1H,br s). [Referential Example 40] 1-Ethyl-2-oxopiperazine hydrochloride [Show Image] 1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Piperazin-2-one (5.07 g) was dissolved in tetrahydrofuran (50 mL) and methanol (50 mL), and, at room temperature, triethylamine (7.76 mL) and di-tert-butyl dicarbonate (12.17 g) were added to the solution, followed by stirring for 4 hours. The reaction solvent was evaporated under reduced pressure, and diethyl ether was added to the residue. The precipitated solid was collected through filtration, to thereby give 3-oxopiperazine-1-carboxylic acid tert-butyl ester as a solid product (9.36 g, 92%). 1H-NMR(400MHz,DMSO-d6)delta:1.40(9H,s), 3.15(2H,br), 3.45(2H,br), 3.81(2H,br), 8.03(1H,br). ESI-MS m/z:201(M+H)+.

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

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1762568; (2007); 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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

109-07-9, Stage-2 : Preparation of 1-CYCLOPROPYL-7- 3-METHYLPIPERAZIN-1-YL)- 6-fluoro-8-methoxy-4-oxo-1, 4-DIHYDRO-3-QUINOLINE carboxylic acid boron difluoride chelate 100 g of Boron difluoride chelate derivative prepared as above in stage-1 is suspended in acetonitrile (800 ml), to that 2-methyl piperazine (44.0 g, 1. 5 mole EQUIV.) IS added and mixed for 15 min to obtain a clear solution. The reaction mass is maintained at 30C – 35C for 12 hrs followed by cooling TO-10C TO-5C. The reaction mass is maintained AT-10C TO-5C for 1 hr. The product is filtered and dried at 45C-50C to constant weight. Dry weight of the product : 116. 0 g (Yield : 93. 9 %).; Stage-2: Preparation of Gatifloxacin (Crude) The boron difluoride chelate derivative (100 g) prepared as above in stage-1 is suspended in acetonitrile (800 ml), 2-methyl piperazine (44 g, 1.5 mole equiv. ) is added and mixed for 15 min to obtain a clear solution. The reaction mass is maintained at 30C- 35C for 12 hrs. Removed the solvent by vacuum distillation. 20% Aq. ethanol (1000 ml) is added, raised the temperature and maintained at 75C to 80C for 2 hrs. The reaction mass is cooled, filtered to remove insolubles. The filtrate is distilled under vacuum to remove solvent completely. Fresh ethanol (250 ml) is added and distilled under vacuum at temperature below 50C. Fresh Ethanol (250 ml) is added to the residue and gradually cooled TO-10C TO-5C. The reaction mass is maintained AT-10C to-5C for 1 hr and filtered. The wet cake is washed with ethanol (30 ML) and dried at 45C-50C to constant weight. The dry weight of the Gatifloxacin is 73.5 g (Yield: 65.4 %)

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; MATRIX LABORATORIES LTD; WO2005/9970; (2005); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: (S)-tert-butyl 4-(3,4-difluorophenyl)-2-methylpiperazine-1-carboxylate A mixture of 4-bromo-1,2-difluorobenzene (1 g, 5.18 mmol), (S)-tert-butyl 2-methylpiperazine-1-carboxylate (1.04 g, 5.18 mmol), t-BuONa (747 mg, 7.77 mmol), BINAP (40 mg, 0.06 mmol) and Pd2(dba)3 (20 mg, 0.02 mmol) in toluene (15 mL) was stirred at 80 C. for 3 hrs. The mixture was then purified by chromatography (silica, EtOAc/PE=1/8) to afford (S)-tert-butyl-4-(3,4-difluorophenyl)-2-methylpiperazine-1-carboxylate (921 mg, 2.95 mmol, 57%) as product. ESI-MS (EI+, m/z): 257.1 [M-55]+.

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); 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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.,70261-82-4

General procedure: A previously described method [19] was followed for the syntheses of 1-5, 7, 8, 10 and 20. Briefly, equimolar quantities of the amine and the acridine/quinoline were dissolved in ethanol, 2 drops of conc. HCl were added and the mixture refluxed for ca 24 h. On cooling, NaOH (1 M) or ammonia solution (25%) was added, followed by dichloromethane to extract the product. Alternatively, if the product precipitated out of solution on alkalinization, it was removed by filtration and purified by column chromatography.

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

Reference£º
Article; Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 2917 – 2929;,
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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

1-tert-butyl 2-methyl 4-(6-Bromo-7-chloro-2-methylquinazolin-4-yl)piperazine- 1,2-dicarboxylate To a solution of 6-bromo-4,7-dichloro-2-methylquinazoline (435 mg, 1.49 mmol) and 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (437 mg, 1.79 mmol in 1,4-dioxane (30 mL), DIEA (769 mg, 5.96 mmol) was added. The mixture was stirred at 80C for 1.5 h. The mixture was allowed to cool to RT and partitioned between water and ethyl acetate. The organic layer was washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash column chromatography on silica gel (5-50 % ethyl acetate/petroleum ether) to afford the desired product (224 mg, 30 % yield) as a yellow solid.

129799-15-1, As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; ARAXES PHARMA LLC; LI, Liansheng; FENG, Jun; WU, Tao; REN, Pingda; LIU, Yi; LIU, Yuan; LONG, Yun, Oliver; WO2015/54572; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Example 13 N2-[4-(dimethylphosphoryl)phenyl]-N4-[4-(4-methylpiperazin-1-yl)benzyl]-5-(trifluoromethyl)pyrimidine-2,4-diamine (0427) (0428) To a solution of 4-chloro-N-[4-(dimethylphosphoryl)phenyl]-5-(trifluoromethyl)pyrimidin-2-amine (prepared as in Example 1: 40 mg, 0.12 mmol) in 2 mL of ethanol was added 50 muL of triethylamine and 4-(4-methylpiperazine)-benzylamine (24 mg, 0.12 mmol). The mixture was microwave at 120 degrees for 20 minutes. The reaction mixture was filtered through a syringe filter and purified by prep-HPLC (Waters Sunfire C18 column with ACN/water mobile phases) to yield a white solid as product (21 mg, 73% yield.) MS/ES+: m/z=519

216144-45-5, As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference£º
Patent; ARIAD PHARMACEUTICALS, INC.; Wang, Yihan; Huang, Wei-Sheng; Liu, Shuangying; Shakespeare, William C.; Thomas, Ranny M.; Qi, Jiwei; Li, Feng; Zhu, Xiaotian; Kohlmann, Anna; Dalgarno, David C.; Romero, Jan Antoinette C.; Zou, Dong; US2015/225436; (2015); 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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

70261-82-4, To a solution of 4-(3-(4-cyanophenyl)imidazo[l,2-a]pyridin-6-yl)benzoic acid (70 mg, 0.206 mmol) in DMF (1.0 mL) were added HATU (117 mg, 0.309 mmol), TV-methyl morpholine (90 mu, 0.824 mmol) and 4-((4-methylpiperazin-l-yl)methyl)aniline (51 mg, 0.309 mmol). The reaction mixture was stirred at room temperature under inert atmosphere for 18 h, then it was diluted with water (15 mL) and extracted with EtOAc (3><30 mL). The combined organic layer was dried over Na2S04 and was concentrated under reduced pressure. The residue was purified by preparative HPLC (CI 8, eluent ACN, water, formic acid 0.1 %) to afford 4-(3-(4- cyanophenyl)imidazo[ 1 ,2-a]pyridin-6-yl)-N-(4-((4-methylpiperazin- 1 - yl)methyl)phenyl)benzamide (40 mg, 37%, AUC HPLC 99%) as a white solid. 1H NMR (400 MHz, CD3OD) delta 8.78 (s, 1H), 8.05 (d, J= 8.4 Hz, 2H), 7.96-7.90 (m, 4H), 7.84 (s, 1H), 7.83 (d, J= 8.4 Hz, 2H), 7.80-7.76 (m, 2H), 7.68 (d, J= 8.8 Hz, 2H), 7.34 (d, J= 8.4 Hz, 2H), 3.56 (s, 2H), 2.70-2.40 (m, 8H), 2.36 (s, 3H); 13C NMR (100 MHz, CD3OD): delta 168.12, 147.47, 141.62, 139.17, 135.76, 134.82, 134.74, 134.53, 134.40, 131.08, 129.56, 129.44, 128.49, 128.30, 127.79, 126.61, 122.95, 122.18, 119.51, 118.48, 112.72, 63.14, 55.55, 53.15, 45.65; MS (ESI) m/z 527 [C33H30N6O + H] +. As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role. Reference£º
Patent; AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH; NACRO, Kassoum; DURAISWAMY, Athisayamani, Jeyaraj; CHENNAMANENI, Lohitha, Rao; WO2013/147711; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

In a sealed tube, 7-fluoro-2-(2-methylimidazo [1 ,2-b]pyridazin-6-yl)-4H-pyrido [1,2- a]pyrimidin-4-one (Intermediate 1; 50 mg, 0.169 mmol), and (R)-2-methylpiperazine (68 mg, 0.677 mmol, 4.0 eq.) were stuffed in DMSO (2 mL) at 110C overnight. The solvent wasremoved under high vacuum. The residue was taken up in CH2C12 and washed with an aqueous saturated solution of NaHCO3. The organic layer was separated and dried over Na2504 and concentrated in vacuo. The crude was purified by column chromatography (5i02, CH2C12/MeOH=95/5 to 90/10) to afford the title product (48 mg, 75%) as a light yellow solid. MS m/z 376.3 [M+H?i.

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; ALSENZ, Jochem; GRASSMANN, Olaf; KUEHL, Peter; METZGER, Friedrich; MCCARTHY, Kathleen Dorothy; MORAWSKI VIANNA, Eduardo Paulo; WOODHOUSE, Marvin Lloyd; (130 pag.)WO2017/80967; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics