Month: September 2020

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 5-bromo-l,2,3-trifluorobenzene (1.05 g, 5.0 mmol), (S) -ter t-butyl 2- methylpiperazine-l-carboxylate (1.0 g, 5.0 mmol), t-BuONa (720 mg, 7.5 mmol), BetaGammaNuAlphaRho (62 mg, 0.1 mmol), and Pd2(dba)3 (92 mg, 0.1 mmol) in dry toluene (20 mL) was stirred for 17 hrs at 80C. The crude product was purified by chromatography (silica, EtOAc/PE = 1/30) to afford (S)-tert- butyl-2-methyl-4-(3,4,5-trifluorophenyl)piperazine-l-carboxylate (0.9 g, 2.7 mmol, 54%) as a yellow oil. ESI-MS (EI+, m/z): 275.0 [M-56]+.

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; (184 pag.)WO2018/89493; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

143673-66-9, (R)-3-Isopropylpiperazine-2,5-dione is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

143673-66-9, Example 153. (2R)-2-(l-Methylethyl)piperazine (153); CH3H3CHNQNH[0540] A solution of (i?)-(-)-3-isopropyl-2,5-piperazinedione (1.0 g, 6.40 mmol) in THF(30 mL) was treated with LAH (25.6 mL, 25.6 mmol, 1.0 M in THF) and warmed to reflux for 16 h. The reaction mixture was then cooled to 0 C and quenched via the addition of water (2 mL), 4 M NaOH (2 mL), and more water (6 mL). On stirring the resultant suspension at it for 1 h, the mixture was dried (Na2SO4), filtered and the filter cake washed with THF (150 mL). The combined filtrates were evaporated to afford the title product as a pale orange semi-solid: 1H NMR deltaH (250 MHz, CDCl3) 2.90 (2H, dd), 2.70 (2H, m), 2.35 (2H, dd), 2.30 (IH, m), 2.22 (2H, br s), 1.48 (IH, m), 0.89 (3H, d), 0.86 (3H, d).

The synthetic route of 143673-66-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PANACOS PHARMACEUTICALS, INC.; NITZ, Theodore, J.; SALZWEDEL, Karl; FINNEGAN, Catherine; WILD, Carl; BRUNTON, Shirley; FLANAGAN, Stuart; MONTALBETTI, Christian; COULTER, Thomas, Stephen; KIMBER, Marc; MAGARACI, Filippo; JOHNSTON, David; WO2008/134035; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 3 4-((4-methyl-1-piperazinyl)methyl)aniline (I-c) Crude I-a (8.5g, 36.2mmol), FeO(OH)/C, 2.0 g as catalyst and 95% ethanol (100 ml) were added into a 500 mL single neck flask, which was refluxed. Into the reaction system were added slowly and dropwise a mixture of 25 mL hydrazine hydrate and 20 mL 95% ethanol. The depletion of the starting materials was confirmed by TLC (methanol: chloroform = 1:15). Suction filtration was performed while the reaction mixture was hot. The filter cake was washed with hot ethanol twice (30 ml *2). After removal of the solvent under reduced pressure, white solid was obtained, which was dried under vacuum to give 6.7 g (I-c); Yield: 90.3%. The product was used for subsequent reaction without further purification. 1H-NMR[300MHz, DMSO-d6]: delta2.1 (3H, s, -CH3), 2.3-2.5 (8H, m, -CH2-*4), 3.5 (2H, s, -CH2-), 4.0(2H, s, -NH2), 7.5 (2H, d, J = 8.7 Hz, ArH), 8.1 (2H, d, J = 8.7 Hz, ArH)., 70261-81-3

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; China Pharmaceutical University; LU, Tao; WANG, Yue; CHEN, Yadong; LU, Yi; WANG, Zhanwei; JIN, Qiaomei; YANG, Taotao; LIN, Guowu; GUO, Qinglong; ZHAO, Li; EP2955185; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

780753-89-1, 1-(4-Fluorophenyl)piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 12^{^-Chloro-S-ttrifluoromethylJphenylJcarbony^-i^-fluorophenyl)^- piperazinone (E12); A solution of 1-(4-fluorophenyl)-2-piperazinone (100 mg, 0.52 mmol, prepared as described below), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (158 mg, 0.82 mmol), and lambda/,lambda/-dimethyl-4-pyridinamine (252 mg, 2.06 mmol) in dichloromethane (4 ml) was stirred at room temperature under argon. 2-Chloro-3- (trifluoromethyl)benzoic acid (116 mg, 0.52 mmol) was added portionwise and the mixture was left overnight. Dichloromethane and aqueous 3N citric acid were then added and the mixture was extracted into dichloromethane (x2). The dichloromethane layers were combined and washed sequentially with water (x1 ), saturated aqueous sodium hydrogen carbonate (x1 ), water (x1 ), and brine (x1 ), and then dried over magnesium sulphate. The solvent was evaporated in vacuo and the crude product was purified by flash-silica gel chromatography, eluting with 30-70percent ethyl acetate in isohexane, to give 4-{[2-chloro-3-(trifluoromethyl)phenyl]carbonyl}-1- (4-fluorophenyl)-2-piperazinone (101 mg) as a white solid. LC/MS [M+H]+ = 401 , retention time = 2.70 minutes.

780753-89-1, The synthetic route of 780753-89-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2009/53459; (2009); 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

A suspension of (3R,4S)-1-benzyl-4-(4-bromophenyl)-N,N-dimethylpyrrolidin-3-amine (3.24 g, 9.02 mmol), 1-(methylsulfonyl)piperazine hydrochloride (2.172 g, 10.82 mmol), tris(dibenzylideneacetone)dipalladium (0) (0.826 g, 0.902 mmol), 2-(dicyclohexylphosphine)-2′,4′,6′-tri-isopropylbiphenyl (0.860 g, 1.803 mmol) and sodium tert-butoxide (2.167 g, 22.54 mmol) in dioxane (32.2 ml) in a 250 ml round bottom flask was taken through three vacuum/nitrogen-purge cycles and heated in a heating block under a condenser at 110C for 2 hours. The mixture was diluted with ethyl acetate and filtered through diatomaceous earth with ethyl acetate washes. The filtrate was washed with saturated sodium bicarbonate (20 ml), dried with magnesium sulfate, filtered, and concentrated. The residue was flash chromatographed (50 mm silica gel column; 6.5% methanol/dichloromethane w/0.1% ammonium hydroxide) to afford the title compound., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Curtin, Michael L.; Pliushchev, Marina A.; Li, Huan-Qiu; Torrent, Maricel; Dietrich, Justin D.; Jakob, Clarissa G.; Zhu, Haizhong; Zhao, Hongyu; Wang, Ying; Ji, Zhiqin; Clark, Richard F.; Sarris, Kathy A.; Selvaraju, Sujatha; Shaw, Bailin; Algire, Mikkel A.; He, Yupeng; Richardson, Paul L.; Sweis, Ramzi F.; Sun, Chaohong; Chiang, Gary G.; Michaelides, Michael R.; Bioorganic and Medicinal Chemistry Letters; vol. 27; 7; (2017); p. 1576 – 1583;,
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.

Step 5: The preparation of 4-(3-Methyl-butyl)-piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester: Piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester (6.0 g, 24.6 mmol) was treated with EtOH (100 mL), isovaleraldehyde (5.3 mL, 50 mmol), and 20% Pd/C (1.0 g), then shaken under an atmosphere of H2. The reaction was filtered and concentrated. The residue was chromatographed on silica gel eluding with 2:1 hexanes/EtOAC to give 7.0 g (90%) of the desired product as an oil. MS: 316 (M+1 for C16H30N2O4); colorless liquid; TLC: SiO2, Rf0.8 (50% hexanes/EtOAc);, 129799-08-2

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

Reference£º
Patent; Warner-Lambert; US6251919; (2001); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Tert-butyl 4-(3-((2,4-dinitrophenyl)amino)propyl)piperazine-l-carboxylateTo a stirred solution of tert-butyl 4-(3-aminopropyl)piperazine-l-carboxylate (2 g, 8.22 mmol), in dichloromethane (DCM) (30 mL) was added l-fluoro-2,4-dinitrobenzene (1.529 g, 8.22mmol) and Et3N (2.291 mL, 16.44 mmol). The reaction mixture was stirred at 25 C for 12 hr. Progress of the reaction was monitored by TLC (TLC system 50% EtOAc in Hexane, Rf :0.5).The reaction mixture was concentrated under reduced pressure to get crude compound as a pale yellow solid. The crude compound was triturated with diethyl ether and dried to afford tert-butyl 4-(3-((2,4-d trophenyl)amino)propyl)piperazine-l-carboxylate (2.7 g, 6.48 mmol, 79 % yield) as a pale yellow solid. LCMS: m/z (M+H = 410).

373608-48-1, 373608-48-1 tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate 17750945, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; BAILEY, James; CHEN, Yao; HURLE, Mark; LEACH, Craig; TURUNEN, Brandon; (103 pag.)WO2018/134731; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

639068-43-2,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.

A solution of potassium carbonate (1.4370 g, 10.40 mmol) in water (3 mL) was added to a mixture of l-N-/-Boc-3,5-dimethyl piperazine (0.6882 g, 3.21 mmol) and mPEG3- Br (0.8872 g, 3.91 mmol) in a vial. The resulting mixture was heated at 120 ¡ãC for 1.5 h by using microwave. The mixture was diluted with water, extracted with dichloromethane (3 x 30 mL). The combined organic solution was washed with brine, dried over brine, concentrated. The residue was dried under high vacuum. The residue was separated with flash column chromatography on silica gel column using 1-5percent methanol/dichloromethane, and NH-column using 0-5percent methanol/ dichloromethane to afford the intermediate.

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; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); 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.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

55121-99-8, A mixture of 0.3 g (1.12 mmol) of the product prepared in step 2.6 and 491 mg (2.24 mmol) of the product prepared in step 2.2 in 6 mL of NMP is placed in a 10 mL microwave tube. The sealed tube is placed in a microwave oven (CEM machine, Discover model) and the mixture is heated under pressure at 120 C. for 60 minutes at a power of 75 W, and then cooled to room temperature. 15 mL of water and then 5 mL of saturated aqueous NaHCO3 are added and the precipitate formed is drained by suction and then dried in an oven. The crude solid is purified by chromatography on a column of silica, eluting with a dichloromethane/methanol gradient (100/0 to 90/10). 0.055 g of the expected product is obtained in the form of an orange powder. m.p.=281 C. %. M+H+=451. Yield=11%. 1H NMR (DMSO-d6, 400 MHz): delta 11.8 (broad s, 1H); 10.3 (s, 1H); 10.2 (d, 1H); 9.0 (s, 1H); 8.0 (broad s, 1H); 7.8 (d, 2H); 7.40 (d, 2H); 7.2 (d, 1H); 4.4 (q, 2H); 3.5 (m, 4H); 3.30 (s, 3H); 2.30 (m, 4H); 1.3 (t, 3H).

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

Reference£º
Patent; SANOFI; US2012/277220; (2012); 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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.,59702-07-7

Preparation of compound 30a: 4-(6-(5-(5-(4-methoxybenzylamino)-l,3,4-thiadiazol- 2-yl)-l-tosyl-lH-indol-3-yl)pyridin-2-yl)-l-methylpiperidin-2-oneA glass microwave reaction vessel was charged with 5-(3-(6-fluoropyridin-2-yl)-l-tosyl- lH-indol-5-yl)-N-(4-methoxybenzyl)-l,3,4-thiadiazol-2-amine (300 mg, 0.512 mmol) and l-methylpiperazin-2-one (117 mg, 1.024 mmol) in NMP (5 mL) followed by Et3N (214\L, 1.537 mmol). The reaction was stirred and heated in an oil bath at 150 ¡ãC for 60 h, and the mixture was diluted with DCM and washed with H20, brine, dried, filtered and concentrated to give the crude product. MS (ESI, pos. ion) m/z: 680 (M+1).

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AMGEN INC.; WANG, Hui-Ling; CEE, Victor, C.; HERBERICH, Bradley, J.; JACKSON, Claire, L., M.; LANMAN, Brian, Alan; NIXEY, Thomas; PETTUS, Liping, H.; REED, Anthony, B.; WU, Bin; WURZ, Ryan; TASKER, Andrew; WO2012/129338; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics