Brief introduction of 120737-78-2

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (Q1a) (500 mg, 1.8 mmol, 1 eq), the corresponding cyclic amine (8.9 mmol, 5 eq) and DMSO (3.6 mL) was heated by microwave irradiation at 115 C for 3 h. The resultant mixture was concentrated by freeze drying, and to the residue was added EtOAc (30 mL). The precipitate was isolated by vacuum filtration and washed with EtOAc, water and Et2O to afford the Boc-protected aminated quinolone.

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Lim, Carine S.Q.; Ha, Kam Pou; Clarke, Rebecca S.; Gavin, Leigh-Anne; Cook, Declan T.; Hutton, Jennie A.; Sutherell, Charlotte L.; Edwards, Andrew M.; Evans, Lindsay E.; Tate, Edward W.; Lanyon-Hogg, Thomas; Bioorganic and Medicinal Chemistry; vol. 27; 20; (2019);,
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Simple exploration of 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-Methyl-4-pyrimidin-2-yl-piperazine- 1 -carboxylic acid tert-butyl ester 100 mg 2-chloro-pyrimidine was added to 175 mg 2-Methyl-piperazine-l -carboxylic acid tert- butyl ester and this mixture was stirred for 2 h at 120 C to give 240 mg of the desired compound. Rt: 1.31 min (method B), (M+H)+: 279, 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; GRAUERT, Matthias; BISCHOFF, Daniel; DAHMANN, Georg; KUELZER, Raimund; RUDOLF, Klaus; WELLENZOHN, Bernd; WO2013/83741; (2013); A1;,
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Downstream synthetic route of 120737-78-2

120737-78-2, As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a stirring mixture of crude acyl chloride 7 (prepared from acid 17 6 (500mg, 1.5mmol)) in anhydrous 93 chloroform (30ml) a solution of 100 (R)-1-Boc-3-aminopyrrolidine (600mg, 3.4mmol) and 101 pyridine (0.6ml, 7.0mmol) in anhydrous chloroform (10ml) was added. The mixture was refluxed for 5min, diluted with chloroform (20ml), washed with aqueous solution of 102 HCl (0.3M), dried and evaporated. The residue was purified by column chromatography on a silica gel in 103 chloroform-methanol (10:0?10:1). The red solid obtained after evaporation was dissolved in hot chloroform (30ml). 104 Methanesulfonic acid (0.3ml, 4.6mmol) was added, the mixture was stirred overnight and evaporated. The residue was dissolved in boiling 105 water (5ml), filtered, the product was precipitated with acetone-ether mixture (3:1). The red solid was collected by filtration, washed with acetone, Et2O, n-hexane and dried.

120737-78-2, As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Article; Shchekotikhin, Andrey E.; Dezhenkova, Lyubov G.; Luzikov, Yuri N.; Treshalin, Michael I.; Shtil, Alexander A.; Preobrazhenskaya, Maria N.; Tsvetkov, Vladimir B.; Volodina, Yulia L.; Tatarskiy, Victor V.; Kalinina, Anastasia A.; Treshalina, Helen M.; Romanenko, Vladimir I.; Kaluzhny, Dmitry N.; Kubbutat, Michael; Schols, Dominique; Pommier, Yves; European Journal of Medicinal Chemistry; vol. 112; (2016); p. 114 – 129;,
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Simple exploration of 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

120737-78-2, 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 4,6-dimethyl-2-(o-tolyl)pyrimidine-5-carboxylic acid (26) (40 mg, 0.17 mmol), tert-butyl 2-methylpiperazine-1-carboxylate45 (50 mg, 0.25 mmol), HOBt(25 mg, 0.18 mmol), EDCI (28 mg, 0.18 mmol) and DIPEA (0.06 mL,0.33 mmol) in DCM (10 mL) was stirred at room temperature for18 h. The solution was then concentrated in vacuo before the residue was purified via silica gel chromatography (1:1 ethyl acetate/hexane) to afford compound 28, a clear oil (45 mg, 65%), as a mixture of conformers. Rf 0.44 (1:1 ethyl acetate/hexane). 1H NMR(CDCl3) d: 7.77e7.74 (m, 1H), 7.34e7.25 (m, 3H), 4.65 (m, 0.5H), 4.51 (m, 0.5H), 4.47 (m, 0.5H), 4.27 (m, 0.5H), 4.02 (m, 0.5H), 3.90 (m,0.5H), 3.40e3.32 (m, 1H), 3.21e2.95 (m, 3H), 2.59 (s, 1.5H), 2.57 (s,1.5H), 2.52 (s, 3H), 2.45 (s, 1.5H), 2.43 (s, 1.5H), 1.46 (s, 9H), 1.27 (d,J6.8 Hz, 1.5H), 1.12 (d, J6.8 Hz, 1.5H). 13C NMR (CDCl3) d: 168.1,167.8, 166.8, 166.8, 163.4, 162.8, 162.4, 154.41, 154.37, 137.9, 137.8,137.4, 137.3, 131.4, 131.43, 131.41, 130.38, 130.36, 129.64, 129.60,126.0, 125.8, 125.4, 80.6, 50.3, 46.9, 46.3, 46.2, 45.5, 41.5, 38.8, 38.0,28.5, 22.55, 22.50, 22.20, 22.15, 21.10, 21.08, 15.6, 15.5. To a solution of tert-butyl 4-(4,6-dimethyl-2-(o-tolyl)pyrimidine-5-carbonyl)-2-methylpiperazine-1-carboxylate (28) (45 mg,0.11 mmol) in DCM (3 mL) was added 10 drops of TFA and allowed to stir at room temperature for 18 h. The volatiles were evaporated to afford the product, a colourless oil (35 mg, quant.) as a mixture of conformers., 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Lim, Zelong; Duggan, Peter J.; Wan, Soo San; Lessene, Guillaume; Meyer, Adam G.; Tuck, Kellie L.; Tetrahedron; vol. 72; 9; (2016); p. 1151 – 1160;,
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Brief introduction of 120737-78-2

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 : To a lOOmL three-necked flask was added 20mL toluene and compound 13a (3g, 0.014mol, l .Oeq), compound 13b (4.3g, 0.022mol, 1.5eq) and t-BuONa (2.064g, 0.022mol, 1.5eq). The reaction was heated to 80oC with nitrogen. Then BINAP (0.3g, 0.42mmol, 0.03eq) and Pd2(dba)3.CHCl3 (0.15g, 0.14mmol, O.OOleq) was added to the stirred mixture . The reaction was heated to reflux for 18h. The solution was cooled, concentrated and extracted with 30 EA from lOmL water. The organic layer was washed with brine , dried , concentrated in vacuum and purified by column chromatography on silica gel eluted with PE: EA= 10: 1 to afford the compound 13c (4g, HPLC: 98%) as a white solid. Yield: 86%.

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LIANG, Congxin; (62 pag.)WO2018/5713; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

Brief introduction of 120737-78-2

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (S) -5- (1- ( (tert-butoxycarbonyl)amino) ethyl) -2- (3- (cyclopropylmethoxy) -4- (difluoromethoxy) phenyl)oxazole-4-carboxylic acid (250 mg, 0.53 mmol) , tert-butyl 2-methylpiperazine-1-carboxylate (130mg, 0.64 mmol) , EDCI (155 mg, 0.80 mmol) and HOAT (182 mg, 1.33 mmol) in DCM(15 mL) was stirred at 0 , and DIPEA (0.37 mL, 2.14 mmol) was added dropwise.After the addition, the mixture was stirred at rt for 5 h and washed with water(10 mL ¡Á 2) . The organic layer was dried over anhydrous Na2SO4and concentrated. The residue was purified by silica gel chromatography elutedwith Petroleum ether/EtOAc (v/v) 2/1 to give the title compound as colorlessthick oil (215 mg, 60) . 1H NMR (400 MHz, CDCl3): delta ppm 7.58 (d, J 8.0 Hz, 1H) , 7.54 (s, 1H) , 7.24 (d, J 8.4 Hz, 1H) ,6.69 (t, JF-H 75.0 Hz, 1H) , 5.27-5.20 (m, 1H) , 4.64-4.43 (m, 3H), 3.96 (d, J 6.7 Hz, 2H) , 3.92-3.89 (m, 1H) , 3.25-3.02 (m, 3H) , 1.54 (d, J 7.0 Hz, 3H) , 1.48 (s, 9H) , 1.41 (s, 9H) , 1.35-1.32 (m, 1H) , 1.22-1.14 (m,3H) , 0.71-0.66 (m, 2H) , 0.41-0.40 (m, 2H) and MS-ESI: m/z 651.3 [M+H] +.

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); A1;,
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Brief introduction of 120737-78-2

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

7-Cyclopentyl-2-(5-formyl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide (1 mol. eq.) and amine (1-2 mol. eq.) are dissolved in either dichloroethane/THF (3:1) or MeOH/dichloromethane mixtures (40 vols.). The mixture is stirred at 20-40C for 16 hours, then cooled to 0C, NaCNBH3 or NaBH4(l .5 – 2 mol. eq.) are then added and the mixture stirred at rt for 5h. Where necessary, further MeOH and/or acetic acid is added to aid reaction progress. The mixture is then quenched with aqueous NaHCO3 solution (10ml) and the product extracted with either diethyl ether, dichloromethane or CHCl3/iPrOH (1 :1). The combined organics are dried (MgStheta4), filtered and the solvent evaporated. The crude product is purified by SiO2 chromatography

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVARTIS AG; ASTEX THERAPEUTICS LTD.; BESONG, Gilbert; BRAIN, Christopher Thomas; BROOKS, Clinton A.; CONGREVE, Miles Stuart; DAGOSTIN, Claudio; HE, Guo; HOU, Ying; HOWARD, Steven; LI, Yue; LU, Yipin; MORTENSON, Paul; SMITH, Troy; SUNG, Moo; WOODHEAD, Steven; WRONA, Wojciech; WO2010/20675; (2010); A1;,
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Some tips on 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 2,6-dichloro-4-cyclopr ile (synthesis described in example 4 step 2, 236 mg, 1 mmol) in N,N-dimethylformamide (10 mL) was added tert- butyl 2-methylpiperazinyl-1-carboxylate (200 mg, 1 mmol), followed by triethylamine (0.14 mL,1 mmol). The mixture was stirred at room temperature for 5 minutes, then diluted with water. The precipitated solid was collected by filtration and dried in an oven to give 4-(6- chloro-3,5-dicyano-4-cyclopropylpyridin-2-yl)-2-methylpiperazinyl-1-carboxylate (330 mg, 82%). LCMS m/z = 301.9 [M+H-Boc]+.

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; ADAMS, Nicholas David; BENOWITZ, Andrew B.; RUEDA BENEDE, Maria Lourdes; EVANS, Karen Anderson; FOSBENNER, David T.; KING, Bryan Wayne; LI, Mei; MILLER, William Henry; REIF, Alexander Joseph; ROMERIL, Stuart Paul; SCHMIDT, Stanley J.; WIGGALL, Kenneth; (1283 pag.)WO2017/216726; (2017); A1;,
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