Month: May 2021

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of methyl (Z)-3-(chloro(4-(methoxycarbonyl)phenyl)methylene)-2- oxoindoline-5-carboxylate (10 mg, 0.03 mmol), N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (81 mg, 0.04 mmol) and TEA (0.5 muL, 0.04 mmol) in EtOH (0.3 mL) was stirred under refluxed for overnight. The reaction solvent was evaporated under reduced pressure, and the residue was purified by column chromatography with dichloromethane/ethanol (50/1, v/v) to obtain the final compound 92 as a yellow solid (9.4 mg, 59% yield): 1H NMR (400 MHz, CDCl3) _ 11.95 (s, 1H), 8.24 (d, J = 8.5 Hz, 2H), 7.93 (s, 1H), 7.74 (dd, J = 8.2, 1.7 Hz, 1H), 7.57 (d, J = 8.5 Hz, 2H), 6.99 (d, J = 8.4 Hz, 2H), 6.94 (dd, J = 8.2, 0.6 Hz, 1H), 6.79 (d, J = 8.6 Hz, 2H), 6.67 (s, 1H), 3.99 (s, 3H), 3.71 (s, 3H), 3.17 (bs, 2H), 2.78 (bs, 2H), 2.38 (bs, 4H), 2.25 (s, 3H), 1.25 (s, 6H)..

262368-30-9, 262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; DALBY, Kevin N.; EDUPUGANTI, Ramakrishna; TALIAFERRO, Juliana; LEE, Juhyeon; (0 pag.)WO2018/160967; (2018); 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.892242-64-7,4-((3-(4-Cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzoic acid,as a common compound, the synthetic route is as follows.,892242-64-7

In a flask, Intermediate 6, Pd/C and hydrazine were mixed and heated for about 4 hours. Reaction mixture was cooled to room temperature and filtered, and then it was redissolved in TFA/DMAc and active charcoal, and then filtered through celite. NaHCO3 was added to neutralize the mixture and the solid was collected by filtration. Compound 12 was purified and dried. It gave about 99% (HPLC, area %) purity. Mass spectra gave [M+1]=525.5. 1H-NMR (300 MHz, DMSO-d6), ppm (delta): 12.36 (1H, s), 8.27 (2H, d), 7.95 (2H, d), 7.85 (2H, t), 7.42 (2H, d), 7.25 (1H, s), 2.96 (4H, m), 2.74 (4H, m), 2.27 (2H, m), 1.57-1.80 (6H, m), 1.06-1.23 (5H, m).

As the paragraph descriping shows that 892242-64-7 is playing an increasingly important role.

Reference：
Patent; VM Oncology LLC; Wu, Jay Jie-Qiang; US2015/218132; (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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

Reference Example 19 A mixture of methyl 4-(tert-butoxycarbonyl)piperazine-2-carboxylate (3.5 g) obtained in Reference Example 16, 3,4,5-trimethoxybenzyl chloride (4.6 g), potassium carbonate (6.0 g) and acetonitrile (80 ml) is refluxed by heating for 10 hours while stirring. The reaction mixture is concentrated under reduced pressure. The concentrate is added to water and extracted with ethyl acetate. The organic layer is washed with water and dried, then the solvent is distilled off under reduced pressure. The residue is purified by means of a silica gel column chromatography (hexane:ethyl acetate = 3:2) to afford methyl 4-tert-butoxycarbonyl-1-(3,4,5-trimethoxybenzyl)piperazine-2-carboxylate as a colorless oily product (5.2 g)., 129799-08-2

As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference：
Patent; Takeda Chemical Industries, Ltd.; EP368670; (1990); 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.78818-15-2,Benzyl 3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1 5-Methoxy-3,6-dihydro-2H-pyrazine-1-carboxylic Acid Benzyl Ester Na2CO3 (45.3 g, 0.43 mol) was added in one portion to a stirred solution of benzyl 3-oxopiperazine-1-carboxylate (5 g, 21.4 mmol) in DCM (200 mL) at 0 C. under N2. The resulting suspension was stirred at 0 C. for 10 min and then trimethyloxonium tetrafluoroborate (11.0 g, 74 mmol) was added in one portion. The resulting mixture was warmed to room temperature and stirred for 6 h before being poured into H2O (200 mL) and separated. The aqueous layer was then extracted with DCM (200 mL). The combined organic extracts were washed with H2O (3*100 mL) and brine (100 mL), dried and concentrated under reduced pressure. The crude residue was further purified by column chromatography on silica using 5% MeOH in DCM as the eluent to give the imino ether (2.5 g, 47%). 1H NMR (360 MHz, CDCl3) delta 2.99 (3H, s), 3.36 (2H, br, s), 3.72 (2H, t, J=5.4 Hz), 4.14 (2H, s), 5.14 (2H, s), 7.28-7.45 (5H, m).

78818-15-2, As the paragraph descriping shows that 78818-15-2 is playing an increasingly important role.

Reference：
Patent; Bryant, Helen Jane; Chambers, Mark Stuart; Jones, Philip; MacLeod, Angus Murray; Maxey, Robert James; US2003/125333; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8,694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: Preparation of N-(3-iodo-4-methylphenyl)-N’-(4-((4-methylpiperazin-1-yl)methyl)-3-trifluoromethylphenyl)urea Triphosgene (1.04 g, 3.5 mmol) and ClCH2CH2Cl (20 mL) were added into a 100 mL round-bottomed flask, and stirred at room temperature until triphosgene was completely dissolved and the system appears colorless and transparent. The reaction system was placed in an ice-salt bath and stirred, 3-iodo-4-methyl aniline (1.64 g, 7 mmol) in ClCH2CH2Cl (20 mL) solution was slowly added dropwise, and the system appears yellow milky. After the addition was complete, the mixture was stirred at room temperature for 4 hours. After the reaction was complete by TLC monitoring, Et3N (1.43 g, 14 mmol) was added, and stirred at room temperature for 0.5 hour. 4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylaniline(1.87 g, 7 mmol) was added and stirred at room temperature for 16 hours, and then the starting materials were monitored by TLC and LC-MS until the reaction was complete. The volatiles were removed by distillation under reduced pressure, and the residue was extracted with ethyl acetate (30 ml x 3) and H2O (30 mL). The organic phases were combined, dried over anhydrous Na2SO4, concentrated and purified by column chromatography, to give a yellow solid. ESI-MS m/z: [M+H]+ = 533.2.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Nanjing Sanhome Pharmaceutical Co., Ltd.; WANG, Yong; ZHAO, Liwen; ZHANG, Wenping; CHEN, Hongyan; BI, Sheng; GAO, Yiping; CHEN, Hongbin; LIU, Yang; XU, Xin; ZHANG, Cang; EP2896620; (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.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-chloroquinazolin-4-yl)piperazine-1,2- dicarboxylate A mixture of 6-bromo-4,7-dichloroquinazoline (300 mg, 1.08 mmol), tert-butyl methyl piperazine-1,2-dicarboxylate (395 mg, 1.62 mmol), DIEA (836 mg, 6.48 mmol) in 1,4-dioxane (8 mL) was stirred at 80C for 1 h. The mixture was allowed to cool to RT, quenched with saturated NaHCO3 solution and then extracted with ethyl acetate. The organic layer was washed with brine, dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by flash column chromatography on silica gel (ethyl acetate/petroleum ether = 1:5) to afford the desired product (367 mg, 70% yield) as a white solid, 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference：
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

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step B: (R)-tert-Butyl 4-(cis-4-(2-chloro-5-nitropyridin-4- ylamino)cyclohexanecarbonyl)-3-methylpiperazine-l-carboxylate. A suspension of cis-4-(2-chloro-5-nitropyridin-4-ylamino)cyclohexanecarboxylic acid hydrochloride (0.5 g, 1.487 mmol) in thionyl chloride (10.86 mL, 149 mmol) was heated at 70C for 1.5 hours. The mixture was concentrated under reduced pressure and dried under high vacuum for 1 hour. The resulting solid was suspended in THF (14.87 mL) and cooled to 0C under nitrogen atmosphere. To this mixture was added (R)-tert-butyl 3- methylpiperazine-l-carboxylate (0.357 g, 1.785 mmol) as a solution in THF (5 mL). The ice bath was removed, and the reaction mixture was stirred overnight at RT. The resulting mixture was diluted with DCM (lOOmL) and washed with saturated aqueous NaHC03 solution (30 mL) and then with saturated aqueous ammonium chloride solution (2x). The organic phase was collected, dried over sodium sulfate, and concentrated under reduced pressure to afford (R)-tert-butyl 4-(cis-4-(2-chloro-5-nitropyridin-4- ylamino)cyclohexanecarbonyl)-3-methylpiperazine-l-carboxylate as a light yellow solid (0.55 g, 77 % yield). MS = 482.2 [M+H]. Calc’d for C22H32C1N505: 481.2.

163765-44-4, As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference：
Patent; AMGEN INC.; BODE, Christiane, M.; CHENG, Alan, C.; CHOQUETTE, Deborah; LEWIS, Richard, T.; POTASHMAN, Michele, H.; ROMERO, Karina; STELLWAGEN, John, C.; WHITTINGTON, Douglas, A.; WO2012/18668; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Part B: 1,1-Dimethylethyl (3R,5S)-3,4,5-trimethyl-1-piperazinecarboxylate. To a solution of 1 ,1-dimethylethyl (3R,5S)-3,5-dimethyl-1-piperazinecarboxylate (2.04 g,9.5 mmol) in dichloromethane (25 ml.) at 0 0C was added formaldehyde (1.075 ml_, 37% water solution, 14.3 mmol) followed by sodium triacetoxyborohydride (2.628 g, 12.4 mmol). The reaction mixture was allowed to warm to room temperature and stirred for 2 h before being diluted with dichloromethane and washed with 1 N NaOH solution. The organics were then washed with brine, dried (MgSO4) and evaporated to yield 1 ,1- dimethylethyl (3R,5S)-3,4,5-trimethyl-1-piperazinecarboxylate (2.06 g, 95%). LCMS: (M+H)+: 229.2.

129779-30-2, 129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/61879; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

25057-77-6, 1,2-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

25057-77-6, A microwave vial was charged with l-bromo-4-chloro-5-fluoro-2- nitrobenzene (0.50 g, 2.0 mmol), 1,2-dimethyl-piperazine (0.39 g, 2.1 mmol), palladium acetate (0.044 g, 0.20 mmol), 4,5-bis(diphenylphosphino)-9,9- dimethylxanthene (0.11 g, 0.20 mmol) and cesium carbonate (2.1 g, 6.4 mmol). The vial was capped, evacuated and backfilled with nitrogen. Toluene (25 mL) was added via syringe and the reaction vial was evacuated and backfilled with nitrogen an additional time. The reaction was warmed to 50 C overnight. The reaction mixture was concentrated onto celite and purified by flash chromatography [0-10% MeOH/DCM + 1% NH4OH] to afford an inseparable mixture of the desired Buchwald product [4-(4-chloro-5-fluoro-2-nitrophenyl)-l, 2-dimethylpiperazine] along with undesired by-product [4-(5-bromo-2-chloro-4-nitrophenyl)-l, 2-dimethylpiperazine]. This mixture was carried forward to the next step where the corresponding products were separable by flash chromatography. LCMS [M+H]+ = 288.3.

25057-77-6 1,2-Dimethylpiperazine 198037, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ZEPEDA-VELAZQUEZ, Carlos Armando; PODA, Gennady; ISAAC, Methvin; UEHLING, David; WILSON, Brian; JOSEPH, Babu; LIU, Yong; SUBRAMANIAN, Pandiaraju; MAMAI, Ahmed; PRAKESCH, Michael; STILLE, Julia Kathleen; (1053 pag.)WO2017/147700; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Sodium hydride (72 mg, 3 [MMOL)] is added to a solution of 7-chloro-4-quinolone (359 mg, 2 [MMOL)] in DMF. After 1 h [AT 40 °C N-PHENYL (TRIFLUOROMETHYLSULFON)] imide (1.0 g, 2.8 [MMOL)] and, 1 h later, 1-tert-butoxycarbonyl-3-methylpiperazine (1.8 g, 8 [MMOL)] is added. The reaction mixture is stirred at 80 [°C] for 2 days, concentrated, diluted with EtOAc, washed with water and brine, dried [(NA2SO4),] and concentrated. The residue is purified by reversed phase HPLC with water-MeCN-TFA to give the title product. 1H NMR (CD3) [8 1.] 0 (d, 3H), 1.5 (s, 9H), 2.9 (m, [1H),] 3.3-3. 8 (m, 6H), 6.9 (d, 1H), 7.5 (m, [1H),] 8.1 (m, 2H), [8.] 8 (d, 1H).

120737-59-9, The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING AKTIENGESELLSCHAFT; WO2004/2960; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics