Heterocyclic Building Blocks-piperazine

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;,
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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);,
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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);,
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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;,
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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;,
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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;,
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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;,
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694499-26-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

Step 12.2: 3-Bromo-4-methyl-N-[4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-benzamide To a solution of 6.1 g (0.025 mol) 3-bromo-4-methylbenzoic acid chloride in 50 mL of acetonitrile are added at 10 C. 7 mL (0.05 mol) triethylamine followed by dropwise addition of a solution of 4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine in 50 mL of acetonitrile (exothermic reaction). The brown suspension is stirred for 5 h at rt and is then allowed to stand over night. Ethyl acetate is added and the solution washed with saturated sodium bicarbonate solution and brine, dried with sodium sulphate and evaporated. Flash-chromatography on silica gel using dichloromethane/ethanol 93:7 containing 1% conc. ammonia gives pure title product: Rf (dichloromethane/ethanol 93:7 with 1% conc. ammonia)=0.4; HPLC tR=3.14 min; MS-ES+: (M+H)+=470, 472.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
Patent; Caravatti, Giorgio; Furet, Pascal; Imbach, Patricia; Martiny-Baron, Georg; Perez, Lawrence Blas; Sheng, Tao; US2006/35897; (2006); A1;,
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70261-82-4,70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

C. 4-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-7-(trifluoromethyl)quinoline A solution of 4-chloro-7-trifluoromethylquinoline (400 mg, 0.0018 M), 1-methyl-4-[(4-aminophenyl)methyl]piperazine (400 mg, 0.0019 M) and 1.4 ml of ethanolic hydrogen chloride in 10 ml of ethanol is heated to reflux, under nitrogen for 15 minutes. The reaction mixture is quenched with ice, neutralized with aqueous 10% sodium hydroxide and extracted with methylene chloride. The methylene chloride solution is washed with water, saturated sodium chloride solution, dried over anhydrous sodium sulfate and concentrated to a white solid. This solid, after recrystallization from ethyl acetate, gives 250 mg (32%) of white crystalline 4-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-7-(trifluoromethyl)quioline of melting point 218-220 C. Anal. Calcd. for C22 H23 F3 N4: Calcd. C, 65.98; H, 5.79; H, 13.99. Found C, 64.82; H, 5.98; N, 13.44.

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

Reference£º
Patent; The Upjohn Company; US4140775; (1979); A;,
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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.,163765-44-4

Example 129: Synthesis of N -(( E )-5-hydroxyadamantan-2-yl)-6-(( R )-2-methylpiperazin-1-yl)picolinamide (Intermediate 10) [325] [326] Step 1: Synthesis of ( R )-tert-butyl 4-(6-((( E )-5-hydroxyadamantan-2-yl)carbamoyl)pyridin-2-yl)-3-methylpiperazine-1-carboxylate [327] 6-Bromo-N-((E)-5-hydroxyadamantan-2-yl)picolinamide(1.0 g, 2.847 mmol), (R)-tert-butyl 3-methylpiperazine-1-carboxylate (855 mg, 4.271 mmol), Pd2(dba)3 (52 mg, 0.057 mmol), xantphos (99 mg, 0.171 mmol), and sodium-tert-butoxide (410 mg, 4.271 mmol) were suspended in toluene (20 ml), and then the resulting liquid was stirred at 100oC under nitrogen stream for 3 hours. A saturated aqueous ammonium chloride solution (20 ml) was added to the resulting reaction liquid, followed by extraction with MC (40 ml x 2). The organic layer was dried over anhydrous sodium sulfate, followed by filtration and concentration, and then the residue thus obtained was subjected to MPLC (90% EtOAc/Hexanes), to obtain 720 mg of pale yellow solid (54%).

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SK Chemicals Co.,Ltd.; RYU, Je Ho; KIM, Shin Ae; RYU, Keun Ho; KIM, Jae Sun; KIM, Nam Ho; HAN, Hye Young; KIM, Yong Hyuk; YOUN, Won-No; LEE, Yoon-Jung; SON, Hyun Joo; LEE, Bong-yong; PARK, Sung Hoon; LEE, Ju Young; LEE, Hyun Jung; JUNG, Hoe Chul; SHIN, Young Ah; LEE, Jung A; LEE, Bo Ram; SA, Joon Ho; WO2011/139107; (2011); A2;,
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