Tag: M.W:200-300

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Tert-butyl (R)-3-(hydroxymethyl)piperazine-1-carboxylate (1.68 g, 7.77 mmol) was added to 113 7-bromo-4,6-dichloro-8-fluoro-3-nitroquinoline (1.2 g, 3.53 mmol), and 56 DIPEA (1.571 ml, 8.83 mmol) in NMP (10 ml) under nitrogen, and the resulting solution was stirred at room temperature for 3 hours. The mixture was partitioned between ethyl acetate and water then the organic layer was washed with water (×2) then brine, dried and evaporated then purified by flash silica chromatography, elution gradient 10 to 40% 57 EtOAc in 58 heptane. Pure fractions were evaporated to dryness to afford 115 tert-butyl (R)-4-(7-bromo-6-chloro-8-fluoro-3-nitroquinolin-4-yl)-3-(hydroxymethyl)piperazine-1-carboxylate (0.96 g, 52%) as a yellow solid. m/z: ES+ [M+H]+ 521., 278788-66-2

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5747-48-8, A solution of but-3-yn-2-one (1 mmol) and PDBTZ (1 mmol), in ethyl acetate (10 mL) is refluxed for two hours. The reaction mixture is washed (water, brine), dried (sodium sulfate), and evaporated. The crude material is purified by flash chromatography to provide the enamine product.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; WO2008/79847; (2008); 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.

General procedure: 4-Nitrobenzyl bromide (46.3mmol) was dissolved in dichloromethane (100mL). The solution was added to the mixture of relative amine (47.0mmol) and triethylamine (70.3mmol) in dichloromethane (20ml). The reaction mixture was stirred at r. t. for 24 h and was extracted with dichloromethane (100ml×3). After removal of the solvent, the residue was crystallized from ethanol, giving yellow powder. Compounds 1 and 2 were used for further reaction without purification. To a suspension of compounds 1-2 (36.2mmol) in 95% ethanol (100ml), 85% NH2NH2·H2O (362mmol), 95% ethanol (100ml) and iron (III) oxide hydroxide (FeO(OH)/C, 2.0g) were added and heated to reflux. When TLC analysis showed complete conversion of the starting material, the reaction mixture was filtrate through Cellit and the filtrate was concentrated in vacuum. The crude product was purified by silica gel colum chromatography (DCM/MeOH) to yield the title compound (3 and 4) as white solid. The mixture of compound 4 (1eq, 18.5mmol), 4-Nitro-1H-pyrazole-3-acid (1.1equiv, 20.4mmol), EDC (1.2equiv, 22.2mmol), HOBT (1.2equiv, 22.2mmol) in DMF (50ml) was stirred for 24h. The ice water (100ml) was added to the reaction mixture. A large amount of yellow solid precipitation (compound 8) was acquired. Compound 8 was used without further purification. Compounds 8 was reduced by the same process as compound 4, and then the resulting compound 12 was purified by column chromatography on silica gel, eluted with the appropriate solvent., 70261-82-4

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

Reference：
Article; Zhi, Yanle; Li, Baoquan; Yao, Chao; Li, Hongmei; Chen, Puzhou; Bao, Jiyin; Qin, Tianren; Wang, Yue; Lu, Tao; Lu, Shuai; European Journal of Medicinal Chemistry; vol. 155; (2018); p. 303 – 315;,
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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of 39 (5.0 g, 13.5 mmol) in DMF (42 mL) were added triethylamine (3.8 mL) and 1-(pyridin-3-ylmethyl)-piperazine (3.2 g, 18.1 mmol) at room temperature under nitrogen. The stirred mixture was heated at 50C for 3 h. The reaction mixture was cooled to room temperature and diluted with water, THF and EtOAc. The organic extract was washed with water, dried over Na2SO4, filtrated and then concentrated. The crude solid was washed with Et2O/EtOAc and filtrated to afford the title compound 40 as a white solid (6.33 g, 12.4 mmol, 91.5%)., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Nagao, Satoshi; Yamane, Yoshinobu; Funasaka, Setsuo; Tanaka, Keigo; Miyazaki, Kazuki; Kotake, Yoshihiko; Kamata, Jun-Ichi; Watanabe-Miyano, Saori; Toyama, Osamu; Ozawa, Yoichi; Mizui, Yoshiharu; Okamoto, Kiyoshi; Ito, Daisuke; Bioorganic and Medicinal Chemistry; vol. 22; 19; (2014); p. 5513 – 5529;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

mCPBA (<77% pure) (5.24 mg, assumed 0.023 mmol) in DCM (0.5 mL) was added to a stirred solution of N- ( 6 - (2,6 -dichlorophenyl ) -2 - (methylthio) -5 -oxo-5 , 6 -dihydropyrido [4 , 3 -d] pyrimidin- 8 - yl) acetamide (8.0 mg, 0.020 mmol) in toluene (1.0 mL) at RT under nitrogen. After 30 min, DIPEA (10.6 muiota, 0.061 mmol) and tert-butyl 4- (4 -aminophenyl ) piperazine-l-carboxylate (6.2 mg, 0.022 mmol) [commercially available] in toluene (0.5 mL) were added, successively, and the temperature was increased to 60 C. After 16 h, the reaction mixture was allowed to cool to RT, and was loaded onto a KP-NH column and purified by flash chromatography (0-100%, EtOAc in cyclohexane) to give the title compound (3.7 mg, 29%) as a yellow solid. LCMS (Method A): RT = 1.39 min, m/z = 624, 626 [M+H]+., 170911-92-9

170911-92-9 tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate 11011301, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ALMAC DISCOVERY LIMITED; O’DOWD, Colin Roderick; ROUNTREE, James Samuel Shane; BURKAMP, Frank; WILKINSON, Andrew John; WO2014/167347; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1403898-64-5, (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 6-(4-fluorobenzyl)-3,3,4-trimethyl-2,3-dihydro-lH-pyrrolo[3,2-b]pyridin-5(4H)-one (190 mg, 0.66 mmol) in DCM (3.00 mL) and was added triethylamine (0.277 mL, 1.99 mmol) and the reaction was stirred at room temperature under an atmosphere of nitrogen. Chloroacetyl chloride (0.058 mL, 0.730 mmol) was added and the reaction was stirred at room temperature for 30 minutes. The reaction was diluted in 25 mL DCM and washed with 10 mL saturated sodium bicarbonate solution, 10 mL water and 10 mL brine. The organic layer was passed through a biotage phase separator and concentrated under vacuum. The residue was dissolved in 3 mL THF and triethylamine (0.28 mL, 1.99 mmol) and (2R,5R)-tert-butyl 5-(hydroxymethyl)-2-methylpiperazine-l- carboxylate (199 mg, 0.86 mmol, obtained as described in WO 2012/143726) was added. The reaction was stirred at 60C for 18h, then was diluted in 25 mL EtOAc and washed with 2 x 10 mL water and 10 mL brine. The organic layer was passed a through biotage phase separator and concentrated under vacuum to afford the title compound (170 mg, 0.31 mmol, 46 % yield). LCMS Method A RT= 0.84 min, ES+ve 557.

1403898-64-5, 1403898-64-5 (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate 71003242, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; CASILLAS, Linda N.; HARLING, John David; MIAH, Afjal Hussain; SMITH, Ian Edward David; RACKHAM, Mark David; (204 pag.)WO2017/182418; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

475272-54-9, (S)-1-Boc-3-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N’N- to carbonyl diimidazole (1.10g, 6.57mmol) in anhydrous DMF (2mL) was added dropwise a solution oftriethylamine (1.10mL, 7.88 mmol) and (S) -1-BOC-3- isopropyl-piperazine (1.00g, 4.38mmol) in anhydrousDMF (2mL) solution at room temperature in a sealed tube 50 min, adding anhydrous methanol (12mL), 80 Cthe reaction 48h, the solvent was removed, a saturated sodium chloride solution (10mL × 3), dried B Acetate(15mL × 2) and the combined organic phases, Na 2 SO 4 dried over anhydrous solvent removed concentratewas separated by column chromatography (leaching Lotion: Petroleumether / EtOAc (v / v) = 4/1), to give339mg of colorless liquid: 4-tert-butoxycarbonyl -2- (S) – isopropyl-piperazin-1-A Methyl, yield: 27%.

475272-54-9, 475272-54-9 (S)-1-Boc-3-Isopropylpiperazine 24820348, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
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 A: To a solution of pentafluorophenol in 520 mL of anhydrous ether at 0 C. there are added in succession 49 g of 1-ethyl-3-(3′-dimethylaminopropyl)-carbodiimide (286 mmol) in portions and 12 mL of formic acid (312 mmol). The whole is stirred at ambient temperature for 2 hours. There is subsequently added a mixture of 32 g of 1-tert-butyl 3-methyl 1,3-piperazinedicarboxylate (130 mmol) and 18 mL of triethylamine (130 mmol) in solution in 520 mL of CH2Cl2. The whole is stirred overnight at ambient temperature. The reaction mixture is hydrolysed with an 1N aqueous HCl solution and extracted with CH2Cl2. The organic phases are subsequently combined and then washed with a saturated aqueous NaHCO3 solution and then with a saturated aqueous NaCl solution until neutral. After drying over MgSO4, filtration and concentration to dryness, the product is isolated by chromatography over silica gel (petroleum ether/AcOEt gradient: 0-30%). The title product is obtained in the form of an oil. IR: nu: C=O: 1674-1745 cm-1 m/z (C12H20N2O5): 272.1 (M+); 295.121 (M+Na)+; 567.253 (2M+Na)+

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

Reference：
Patent; Le Diguarher, Thierry; Casara, Patrick; Starck, Jerome-Benoit; Henlin, Jean-Michel; Davidson, James Edward Paul; Murray, James Brooke; Graham, Christopher John; Chen, I-Jen; Geneste, Olivier; Hickman, John; Depil, Stephane; Le Tiran, Arnaud; Nyerges, Miklos; De Nanteuil, Guillaume; US2015/51189; (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.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 4-(2-chloroethyl)piperazine-l -carboxylate (9.7 g, 38.9 mmol) in ethanol (25 ml) was added hydrazine hydrate (19.5 ml, 38.9 mmol) and resulting recation mixturte was heated to 60 C for 3h. The solvent was evaporated under reduced pressure, diluted with water, extracted with diethyl ether (75 ml x 4) and the organic extract was dried over Na2S04 and concentrated under reduced pressure to give 9.6 g of the desired product as colorless oil. lH NMR (400 MHz, DMSO-ifc): delta 1.45 (s, 9H), 2.38-2.45 (m, 4H), 2.52 (t, J = 6.0 Hz, 2H), 2.88 (t, J = 6.0 Hz, 2H), 3.04 (br, s, 3H), 3.39-3.69 (m, 4H).

208167-83-3, 208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GLENMARK PHARMACEUTICALS S.A.; KUMAR, Sukeerthi; CHAUDHARI, Sachin Sundarlal; GHARAT, Laxmikant Atmaram; KHAIRATKAR-JOSHI, Neelima; SHAH, Daisy Manish; MUKHOPADHYAY, Indranil; (327 pag.)WO2018/203298; (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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To the chloro compounds (1.00 mmol) in toluene, were added piperazines 8a-j (1.0 mmol) at room temperature. The reaction mixture was heated at 110 oC for overnight. After completion (TLC), the reaction mixture was extracted with ethyl acetate and water. The organic layer was separated and dried over anhydrous Na2SO4, evaporated to dryness. The residue was purified with column chromatography using an eluent of 25% ethyl acetate in hexane to furnish the compounds with moderate to good yields (64-82%).

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference：
Article; Banu, Saleha; Bollu, Rajitha; Naseema, Mohammad; Gomedhika, P. Mary; Nagarapu, Lingaiah; Sirisha; Kumar, C. Ganesh; Gundasw, Shravan Kumar; Bioorganic and Medicinal Chemistry Letters; vol. 28; 7; (2018); p. 1166 – 1170;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics