Month: April 2021

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.,59878-57-8

INTERMEDIATE 46(S)-N-(I – (2- r4-(Cyclopropanecarbony?piperazin- 1 -yl] -8-methylquinolin-3 -yl) ethvD- 2,2,2-trifluoroacetamideIntermediate 45 (100 mg, 0.32 mmol), cyclopropyl(piperazin-l-yl)methanone (0.09 mL, 0.63 mmol), NMP (2 mL) and DIPEA (0.10 mL, 0.80 mmol) were combined in a sealed tube and heated to 1400C for 4 days. After cooling, Et2O (50 mL) was added to the reaction mixture. The organic layer was washed with water (5 x 50 mL) and brine. The organic layer was dried (MgSO4), filtered and the solvent was removed in vacuo. Purification by column chromatography on silica, eluting with 0-30% EtOAc in isohexane, gave the title compound (82 mg, 60%) as a pale yellow gum. delta? (CDCl3) 8.01 (IH, s), 7.75-7.65 (IH, m), 7.59 (IH, d, J 8.1 Hz), 7.55-7.48 (IH, m), 7.40-7.31 (IH, m), 5.58-5.47 (IH, m), 4.00-3.86 (3H, s), 3.85-3.72 (IH, s), 3.54-3.30 (2H, m), 3.18 (2H, m), 2.71 (3H, s), 1.84-1.76 (IH, m), 1.64 (3H, d, J6.8 Hz), 1.09-0.97 (2H, m), 0.84-0.75 (2H, m).

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Patent; UCB PHARMA S.A.; ALLEN, Daniel, Rees; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MACDONALD, Jonathan, David; MATTEUCCI, Mizio; NASH, David, John; OWENS, Andrew, Pate; RAPHY, Gilles; SAVILLE-STONES, Elizabeth, Anne; SHARPE, Andrew; WO2010/100405; (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.5521-38-0,2-(4-(4-Nitrophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

5521-38-0, General procedure: The substituted nitro compound 11 (1 equiv in a mixture of EtOH-H2O, 95:5, 20mL) was treated with 10% Pd-carbon (5% w/w). The reaction was subjected to hydrogenation under hydrogen gas at room temperature and the reaction was monitored by TLC. After completion of the reaction, the mixture was filtered through a Celite bed and concentrated in a vacuum to afford product 12.

5521-38-0 2-(4-(4-Nitrophenyl)piperazin-1-yl)ethanol 2763936, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Hou, Yunlei; Zhu, Liangyu; Li, Zhiwei; Shen, Qi; Xu, Qiaoling; Li, Wei; Liu, Yajing; Gong, Ping; European Journal of Medicinal Chemistry; vol. 163; (2019); p. 690 – 709;,
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.53788-49-1,tert-Butyl 4-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

53788-49-1, Example 2 Preparation of Intermediate 4-(4-chloro-pyrimidin-2-yl)-piperazine-1-carboxylic Acid Tert-Butyl Ester (I-2a): To a suspension of 2,4-dichloropyrimidine (1.00 g, 6.71 mmol) in 13.4 mL of toluene was added 4-methyl-piperazine-1-carboxylic acid tert-butyl ester (1.34 g, 6.71 mmol). The reaction was heated to reflux overnight, then cooled to room temperature and concentrated in vacuo. The residue was taken up in 20 mL of water and extracted with ethyl acetate (2*40 mL). The combined organic layers were washed with brine (25 mL), then dried over sodium sulfate, filtered, and concentrated in vacuo to an off-white solid. Flash column chromatography (silica gel, gradient elution from 5% ethyl acetate-hexanes to 20% ethyl acetate-hexanes) yielded 1.14 g of the title compound (I-2a). 1H NMR (400 MHz, CDCl3) delta 8.15 (d, 1H); 6.52 (d, 1H); 3.80 (m, 4H); 3.48 (m, 4H); 1.47 (s, 9H). MS (APCI+) Calc: 298, Found: 299.1 (M+1).

The synthetic route of 53788-49-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chiang, Phoebe; Novomisle, William A.; Welch JR., Willard M.; US2003/105106; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

21655-48-1, A mixture of 2,5-dibromo-4-methylpyridine (3.5 g, 18.42 mmol), Hunig’s Base (9.63 mL,55.26 mmol) and (2R,6S)-2,6-dimethylpiperazine (2.314 g, 20.26 mmol) in DMSO (55 mL) was stirred at 110 ¡ãC for 18 hours. The reaction mixture was diluted with EtOAc (75 mL), and washed sequentially with water (2 x 50 mL) and saturated brine (25 mL). The organic layer was dried over MgSO4, filtered and concentrated to afford the crude (3S,5R)-1-(5-bromo-4-methylpyridin-2-yl)-3,5-dimethylpiperazine as an oil which crystallised on suanding to give a pale yellow solid (5.05 g, 96percent). Used with no further purification.

The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Holmes, Jane L.; Almeida, Lynsie; Barlaam, Bernard; Croft, Rosemary A.; Dishington, Allan P.; Gingipalli, Laksmaiah; Hassall, Lorraine A.; Hawkins, Janet L.; Ioannidis, Stephanos; Johannes, Jeffrey W.; McGuire, Thomas M.; Moore, Jane E.; Patel, Anil; Pike, Kurt G.; Pontz, Timothy; Wu, Xiaoyun; Wang, Tao; Zhang, Hai-Jun; Zheng, Xiaolan; Synthesis; vol. 48; 8; (2016); p. 1226 – 1234;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Acetic acid (5.76 g, 96 mmole) was added to a suspension of aldehyde (10 g, 24 mmole) and piperazine (6.91 g, 48 mmole) in NMP (150 mL). The reaction was stirred at room temp for 16h then treated with NaB (OAc) 3H (12.7 g, 60 mmole). The reaction was stirred at room temp for 20h during which time the reaction becomes very viscous. 1N NAOH (200 mL) was then added and the reaction was stirred for LH. The reaction was then poured onto H20 (750 mL) and filtered. The solid was washed with HO (2 x 350 mL), ETOH (100 mL), and ET20 (200 mL). The solid was then dried under vacuum to yield the desired amine as the free base (9.98 g, 76%).

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GPC BIOTECH, INC.; WO2004/92139; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

76003-29-7, A mixture of 1 ,1 -dimethylethyl 3-oxo-1 -piperazinecarboxylate (0.489 g, 2.44 mmol), 3-bromothiophene (0.332 g, 2.036 mmol), copper(l) iodide (0.019 g, 0.102 mmol), potassium carbonate (0.563 g, 4.07 mmol) and trans-N,N-dimethyl-cyclohexane-1 ,2- diamine (0.029, 0.204 mmol) in 1 ,4-dioxane (5 mL) was heated at reflux under nitrogen for 24 hours. After cooling to room temperature, the reaction mixture was filtered through silica ge. eluting with DCM:EtOAc/1 :1 , The filtrate was concentrated and the residue was purified by silica gel chromatography to afford 1 ,1 -dimethylethyl 3-oxo-4-(3-thienyl)-1 – piperazinecarboxylate (0.305 g, 53%) as a white solid.

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; PEAT, Andrew, James; PRICE, Daniel, J.; SHOTWELL, John, Brad; TAI, Vincent; ZHANG, Huichang; WO2011/41713; (2011); 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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

Preparation 2 Benzyl 4-(2-Hydroxyethyl)piperazine-1-carboxylate A 250 mL round bottomed flask was charged with N-(2-hydroxyethyl)piperazine (3.00 g, 24.4 mmol) followed by anhydrous THF (150 mL) and triethylamine (3.40 mL, 24.4 mmol). The resulting solution was cooled to 0 C. and a solution of benzyl chloroformate (3.10 mL, 21.8 mmol) in anhydrous THF (10 mL) was slowly added via syringe resulting in the formation of a cloudy white suspension. This suspension was stirred at 0 C. for 30 minutes, then allowed to warm to room temperature with stirring over 3 h. The reaction mixture was then concentrated under reduced pressure. Purification of the residue by silica gel chromatography, eluding with 5% MeOH in CH2Cl2, afforded 5.76 g (100%) of Preparation 2 as a colorless oil. Rf=0.60 (SiO2, 5% MeOH in CH2Cl2). 1H NMR (500 MHz, CDCl3): delta=7.34 (m, 5H), 5.13 (s, 2H), 3.62 (t, J=5.2 Hz, 2H), 3.52 (t, J=5.2 Hz, 4H), 2.64 (br s, 1H), 2.55 (t, J=5.2 Hz, 2H) and 2.47 (br s, 4H). m/z=265 [M+H]+., 103-76-4

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Bristol-Myers Squibb Company; US2007/88029; (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.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

55121-99-8, Step 2.2: {4-[7-(3,5-Difluoro-4-morpholin-4-ylmethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino]-phenyl}-(4-methyl-piperazin-1-yl)-methanone (2) In a sealed tube, 2-chloro-7-(3,5-difluoro-4-morpholin-4-ylmethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidine (50.0 mg, 0.130 mmol), (4-Amino-phenyl)-(4-methyl-piperazin-1-yl)-methanone (42.1 mg, 0.182 mmol), KOtBu (21.1 mg, 0.182 mmol) and SK-CC02-A (12.5 mg, 0.020 mmol, Pd catalyst 2-(Dimethylaminomethyl)-ferrocen-1-yl-palladium(II)-chlorid Dinorbornylphosphin Complex, Fluka No. 44696) are suspended in THF (2 ml) under Ar. The reaction mixture is stirred at 80 C. for 1.5 h, cooled to rt, and then filtered through a Celite plug. The filtrate is concentrated under reduce pressure. The residue is purified by reverse phase prep-HPLC (Waters) to afford the title compound (2) as a white solid. HPLC: tR=0.89 min (Method A); MS-ES: (M+H)+=548.

As the paragraph descriping shows that 55121-99-8 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; US2009/203688; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1 In a 100 ml four-neck flask, 5.00 g (= 0.0499 mole) of racemic 2-methylpiperazine was placed, and 44 g of 1-butanol (water content 0.05 wt%) was added for dissolution. The solution was cooled to 0C, and 8.47 g of benzyl chlorocarbonate (= 0.0489 mole, purity by HPLC determination analysis 98.5 wt%, 0.98 molar time) was added dropwise in a liquid temperature range from 0 to 8C. Then, stirring was carried out at 0 to 5C for 2 hours, and the reaction solution was partially sampled and determined by the internal standard method (internal standard: anisole). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 83.9% (based on the amount of 2-methylpiperazine). The reaction solution was further stirred at room temperature for 12 hours and analyzed. As a result, the reaction yield was 85.1%. Example 3 A reaction was performed as described for Example 1, except that the amount of benzyl chlorocarbonate used was changed from 8.47 g to 10.1 g (= 0.0597 mole, 1.17 molar times). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 93.8% (based on the amount of 2-methylpiperazine) after lapse of 2 hours at 0 to 5C. Stirring was carried out at room temperature for further 12 hours, being followed by analysis. As a result, the reaction yield was 95.1%.

109-07-9, 109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (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.438049-91-3,(3R,5R)-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,438049-91-3

A mixture of (3S,5R)-tert-butyl 3,5-dimethylpiperazine-l-carboxylate (2.14g, 10.0 mmol), 3-bromopropan-l-ol (2.76 g, 20 mmol) and K2C03(2.76 g, 20 mmol) in DMF (5.0 mL) was heated to 90C for 2 h in a microwave. The reaction mixture was poured into water (30 mL) and extracted with EtOAc. The organic phase was separated, dried and concentrated. The residue was purified by chromatography (DCM:MeOH=30: 1) to provide (3R,5S)-tert-butyl 4-(3- hydroxypropyl)-3,5-dimethylpiperazine-l-carboxylate as a yellow liquid (2.14g, 50%).

438049-91-3 (3R,5R)-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 51670829, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PRINCIPIA BIOPHARMA INC.; BRAMELD, Kenneth Albert; VERNER, Erik; (122 pag.)WO2016/191172; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics