Month: April 2021

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: Carbonyldiimidazole (0.97g, 0.006mol) in 5mL of dry THF was added to a solution of intermediates 1 (1.11g, 0.006mol), 2 (1.19g, 0.006mol), 3 (1.19g, 0.006mol) or 4 (1.28g, 0.006mol) dissolved in 10mL of anhydrous THF while stirring. After the end of gaseous (carbon dioxide) evolution (c.a. 0.5h), the respective secondary amines (0.006mol) dissolved in 5mL of anhydrous THF was added dropwise. The mixture was stirred at room temperature (approx. 24h) and evaporated to dryness. The crude product was purified by column chromatography (dichloromethane/methanol, 9:0.3, v/v). The final amides were obtained as solid substances followed by concentration of organic solvents under reduced pressure, and recrystallization from 2-propanol.

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

Reference£º
Article; Kami?ski, Krzysztof; Zagaja, Miros?aw; Rapacz, Anna; ?uszczki, Jarogniew J.; Andres-Mach, Marta; Abram, Micha?; Obniska, Jolanta; Bioorganic and Medicinal Chemistry; vol. 24; 4; (2016); p. 606 – 618;,
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

General procedure for Buchwald-Hartwig couplingIn a oven dried 20 mL round-bottomed flask 2,2′-bis(diphenylphosphino)-l,l’-binaphthyl (racemic) (0.07 g, 0.1 12 mmol) and palladium(II) acetate (0.02 g, 0.089 mmol) in dry toluene (3 ml) were added under N2 atm. followed by addition of (2No.,6S)-2,6-dimethylpiperazine (0.101 g, 0.888 mmol), 12a (0.2 g, 0.740 mmol) and cesium carbonate (0.338 g, 1.037 mmol). Reaction mixture was stirred at 100 ¡ãC for 16 h. After 16 h reaction mixture was cooled, diluted with EtOAc and filtered through celite pad, filtrate was concentrated and purified by column chromatography with a silica gel column and was eluted with 15 percent MeOH in CHC to obtain a pure product 13a, 0.1 g (45 percent)

21655-48-1, 21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CAMBRIDGE ENTERPRISE LIMITED; GLEN, Robert; HILEY, Robin; BELL, James; SPRING, David; KAPADNIS, Prashant, Bhimrao; WO2011/98776; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

674792-05-3, (S)-1-Boc-2-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,674792-05-3

[00339] To a solution of (5)-tert-butyl 2-isopropylpiperazine-1-carboxylate (400 mg, 1.76 mmol) in anhydrous toluene (10 mL) was added methyl 4-bromo-2-(methylsulfonyl)benzoate (1.03 g, 4.8 mmol), X-phos (80 mg, 0.17 mmol), Cs2CO3 (1.50 g, 4.62 mmol) and Pd2(dba)3 (200 mg, 0.22 mmol) under N2. The reaction mixture was stirred at 100 oC overnight. The reaction was quenched with water (20 mL), and extracted with EtOAc (4 X 20 mL). The combined organic layers were dried over anhydrous Na2504, filtered, concentrated and then purified by preparative TLC with petroleum ether / EtOAc 5/1 to afford (5)-tert-butyl 2- isopropyl-4- (4- (methoxycarbonyl)-3- (methylsulfonyl)phenyl)piperazine- 1 -carboxylate (500 mg, 65% yield) as a grey solid.

As the paragraph descriping shows that 674792-05-3 is playing an increasingly important role.

Reference£º
Patent; VITAE PHARMACEUTICALS, INC.; CLAREMON, David, A.; DONG, Chengguo; FAN, Yi; LEFTHERIS, Katerina; LOTESTA, Stephen, D.; SINGH, Suresh, B.; TICE, Colin, M.; ZHAO, Wei; ZHENG, Yajun; ZHUANG, Linghang; (185 pag.)WO2016/22521; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4318-42-7

To a vial was added 4-fluoronitrobenzene (1.41 g, 1.06 mL, 0.01 mo1) , N,N-diisopropylethylamine (1.92 mL, 0.011 mmol), isopropylpiperazine (1.41g, 0.011 mmol), and N1N- dimethylformamide (10 mL) . Mixture was heated at 1000C for 48 h in a sealed tube. The reaction mixture wag cooled to room temperature and concentrated. The residue was purified via silica gel column chromatography (gradient elution with 0 to 10percent methanol in dichloromethane) to afford 1-isopropyl- 4- (4-nitrophenyl)piperazine.

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AMGEN INC.; WO2006/44823; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of isocyanate (1.877mmol) in toluene (2.5mL) was added a solution of a monosubstituted piperazine (1.877mmol) in toluene (1.0mL). The reaction mixture was heated at 40-45C for 30 to 60min. The reaction mixture was then cooled down to room temperature (22-25C) and the resulting solids were filtered and washed with more toluene (2.0mL). The wet solids were then placed in 2.0mL of toluene, stirred at room temperature for about 30min, filtered and washed with toluene (1.0mL) to obtain the crude disubstituted piperazine derivative. Finally, all crude derivatives were purified by silica-gel column chromatography using a mixture of dichloromethane/methanol (9:1) to afford pure piperazines products.

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Article; Patil, Mahadev; Noonikara Poyil, Anurag; Joshi, Shrinivas D.; Patil, Shivaputra A.; Patil, Siddappa A.; Bugarin, Alejandro; Bioorganic Chemistry; vol. 92; (2019);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7,4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of 4-fluorobenzaldehyde (0.017 mol, 1.82 mL) and an appropriate secondary aminein DMF (10 mL) was refluxed (0.017 mol) in the presence of potassium carbonate (K2CO3, 0.017 mol,2.35 g). After completion of reaction, the mixture was cooled with ice-water (10 mL) and extractedwith ethyl acetate (3 20 mL). The ethyl acetate phases were combined, and the remaining productwas collected after evaporation of the solvent. The following compounds were prepared in this way:4-(4-methylpiperazin-1-yl)benzaldehyde (1a), CAS No:27913-99-1, Yield 82percent, m.p. = 55?57 ¡ãC (measured),m.p. = 58?60 ¡ãC (reported) [60]; 4-(4-ethylpiperazin-1-yl)benzaldehyde (1b), CAS No:197638-76-9,Yield 79percent, obtained as an oil; 4-(4-isopropylpiperazin-1-yl)benzaldehyde (1c), CAS No:197638-78-1,Yield 84percent, obtained as an oil and 4-(4-cylopropylpiperazin-1-yl)benzaldehyde (1d), CAS No:1292778-23-4,Yield 78percent, obtained as an oil.

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Tokgoez, Gamze; Oezkay, Uemide Demir; Osmaniye, Derya; Yuecel, Nazl? Turan; Can, Oezguer Devrim; Kaplanc?kl?, Zafer As?m; Molecules; vol. 23; 11; (2018);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5521-39-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5521-39-1,2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of compound 7, 8, or 9 (1 equiv) in 1-butanol was added compounds 12(1.1 equiv) and p-toluenesulfonic acid (1 equiv). The mixture was placed in a pressure flask, and heated to 100C for 15h. The reaction mixture was quenched by saturated Na2CO3 aqueous solution, and then was extracted with DCM and the organic phase was washed with water, dried over anhydrous Na2SO4. The combined organic layer was concentrated under reduced pressure and was further purified by flash column chromatography using dichloromethane/methanol as eluent to afford product H1-H14, Y1-Y14, or L1-L14 as a pale yellow solid.

5521-39-1 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol 767100, 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.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step C. 2-Ethyl-N-(3-fluoro-4-piperazin-1-yl-phenyl)-butyramide. To a solution of 4-(4-amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (2.0 g, 8.9 mmol) and Et3N (1.4 mL, 10.0 mmol) in DCM (60 mL) was added 1-ethylbutyryl chloride (1.4 mL, 10.0 mol). The mixture was stirred for 18 h, quenched with 1 N NaHCO3 (50 mL), and extracted with DCM (3*50 mL). The organic layers were combined, dried (Na2SO4), and concentrated. Chromatography of the residue (SiO2; EtOAc/hexanes) gave 4-[4-(2-ethyl-butyrylamino)-2-fluoro-phenyl]-piperazine-1-carboxylic acid tert-butyl ester. Step A. 4-[4-(2-Ethyl-butyrylamino)-2-fluoro-phenyl]-piperazine-1-carboxylic acid tert-butyl ester. To a solution of 4-(4-amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (2.96 g, 10.0 mmol) and TEA (1.52 g, 15.0 mmol) in DCM (60 mL) was added 2-ethyl butyryl chloride (2.08 g, 15.0 mmol). After 18 h, the mixture was diluted with DCM (50 mL) and washed with satd. aq. NaHCO3 (1¡Á30 mL) and water (2¡Á30 mL). The organic layer was dried (Na2SO4) and concentrated. The residue was purified (SiO2; acetone/DCM and EtOAc/DCM) to yield the title compound (2.00 g, 51%). 1H NMR (CDCl3): 7.55-7.45 (m, 1H), 7.15 (br s, 1H), 7.14-7.08 (m, 1H), 6.86 (t, J=9.0, 1H), 3.62-3.54 (m, 4H), 3.01-2.93 (m, 4H), 2.04-1.96 (m, 1H), 1.76-1.65 (m, 2H), 1.60-1.50 (m, 2H), 1.48 (s, 9H), 0.94 (t, J=7.4, 6H).; Step A. 4-[4-(2-Ethyl-butyrylamino)-2-fluoro-phenyl]-piperazine-1-carboxylic acid tert-butyl ester.; To a solution of 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylic acid-tert-butyl ester (3.11 g, 10.5 mmol) and TEA (1.60 g, 15.8 mmol) in DCM (50 mL) was added 2-ethylbutyryl chloride (2.17 mL, 15.8 mmol) slowly. After 18 h, the mixture was washed with water, dried (Na2SO4), and concentrated. The residue was purified twice [SiO2; 1) acetone/DCM, 2) EtOAc/hexanes] to give the title compound. (2.07 g, 50%)., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Bonaventure, Pascal; Carruthers, Nicholas I.; Chai, Wenying; Dvorak, Curt A.; Jablonowski, Jill A.; Rudolph, Dale A.; Seierstad, Mark; Shah, Chandravadan R.; Swanson, Devin M.; Wong, Victoria D.; US2007/100141; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Racemic ulifloxacin (105 g) was dissolved in DMSO (1500 mL). D-tartrate (27 g) solution in DMSO (405 mL) was added to the racemic ulifoxacin solution with agitation. Cloudiness and precipitation appear. After 20 hours of agitation at an ambient temperature, the mixture was filtered. The solid was dried under vacuum to yield 86 g of solid. The solid was recrystallized in DMSO to yield 37 g of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a] quinoline-3-carboxylic acid-D-tartrate salt; the elemental analysis indicates: C 49.08%, H 5.06%, N 9.50%, and S 7.44% (corresponding to: C16H16FN3O3S¡¤1/2C4H6O6¡¤H2O, calculated value: C 48.86%, H 4.78, N 9.50%, and S 7.25%). The salt was dispersed in water and the dispersion was neutralized witrh 2% NaOH aqueous solution to a pH value of 7 to 8. The precipitate is filtered and dried to yield 24.5 g of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeta[3,2-a]quinoline-3-carboxylic acid. It has a rotation [Show Image] (c = 0.15, 0.1 mol/L NaOH), 1H-NMR (DMSO-d6) delta2.11(3H, d, j=6.2 Hz), 2.85?3.20 (8H, m), 6.40(1H, q, j=6.2 Hz), 6.89(1H, d, j=7.4Hz), 7.79(1H, d, j=13.9 Hz), optical purity e.e.>95%.

112984-60-8, The synthetic route of 112984-60-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangzhou Baiyunshan Pharmaceutical Co. Ltd. Guangzhou Baiyunshan Pharmaceutica Factory; Guangzhou Pharmaceutical Industry Academe; EP2258705; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 6- fluoro- 1 -methyl-4-oxo-7-(piperazin- 1 -yl)- 1 H,4H- [1,3] thiazeto[3 ,2-a]quinoline-3-carboxylic acid (690 mg, 1.98 mmol) in DMF (10 ml), triethylamine (0.55 ml, 3.95 mmol) and compound B(500 mg, 1.97 mmol) were added and the reaction mixture was stirred at room temperature for 18 h. Aftercompletion of the reaction excess ethyl acetate was added into the reaction mixture and solids were filtered out. The crude obtained after concentrating the filtrate, was purified by flash column chromatography over silica gel using 8% methanol-DCM eluent to obtain 18 (135 mg, 13%) 1H NMR (DMSO-d6): oe 14.65 (brs, 1H, COOH), 13.09 (brs, 1H, NH), 8.47-8.35 (m, 1H, ArH), 8.12- 8.08 (m, 1H, ArH), 7.79 (d, 1H, JAB = 13.5 Hz, ArH), 7.65 (d, 1H, JAB = 8.5 Hz, ArH), 6.92 (d, 1H,JAB = 7.0 Hz, ArH), 6.37 (q, 1H, JAB = 5.5 Hz,SCHN), 3.91 (s, 2H, CH2), 2.76-2.62 (m, 4H, CH2N),2.01 (d, 3H, J = 6.0 Hz, CH3). ESI-MS (mlz): 525.07 (M+H)., 112984-60-8

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; GHOSH, Shamik; GHOSH, Sumana; SINHA, Mau; SADHASIVAM, Suresh; BHATTACHARYYA, Anamika; MAVUDURU, Siva Ganesh; TANDON, Nupur; KUMAR, Deepak; (149 pag.)WO2017/17631; (2017); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics