Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

General procedure: General procedure for the synthesis of 15b-15u. To a solution ofcompound 13a (0.41 g, 1.06 mmol) in 2-butanol (5 mL), 1-(2-(dimethylamino)ethyl)-1H-pyrazol-4-amine (0.196 g, 1.27 mmol)and trifluoroacetic acid (94 mL) were added in a sealed tube. Thereactionwas heated at 95 C for 18 h. The reaction mixturewas thenallowed to cool to room temperature. The mixture was transferredto a round-bottom flask and then the solvent was removed underreduced pressure. The residue was dissolved in DCM (2.0 mL) andTFA (2.0 mL), and the resulting mixture was stirred for 5 h at roomtemperature. The solvent was removed under reduced pressure,and the residue was neutralized with saturated NaHCO3 aqueoussolution. The water layer was extracted with DCM. The organiclayer was combined and washed with brine, dried over Na2SO4,filtered, concentrated, and purified by silica gel chromatography toafford 15a as a yellow solid (0.264 g, 65% for two steps)., 122833-04-9

The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Yu, Lei; Huang, Minhao; Xu, Tianfeng; Tong, Linjiang; Yan, Xiao-e; Zhang, Zhang; Xu, Yong; Yun, Caihong; Xie, Hua; Ding, Ke; Lu, Xiaoyun; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 1107 – 1117;,
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142-64-3, Piperazine Dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound, 2 (250 mg, 1.23 mmol) was taken in THF, and piperazinedihydrochloride (199 mg, 1.25 mmol) and K2CO3 (690mg, 5 mmol) were added. The reaction mixture was refluxed overnight.After complete reaction the solvent was removed under reduced pressure and theprecipitate obtained was washed with water and hexane (5 x 3ml). The crudeproduct was purified by column chromatographyusing gradient of ethylacetate andhexane (20 % v/v) to obtain off white color compound. Yield 80 % (250mg). M.p. 91-92C. 1H NMR(300 MHz, CDCl3) delta (ppm): 7.38-7.12 (m, 10 H), 4.21 (s, 1H),2.40 (Br, 8 H).

142-64-3, As the paragraph descriping shows that 142-64-3 is playing an increasingly important role.

Reference£º
Article; Srivastava, Priyanka; Ali, Rashid; Razi, Syed S.; Shahid, Mohammad; Patnaik, Satyakam; Misra, Arvind; Tetrahedron Letters; vol. 54; 28; (2013); p. 3688 – 3693;,
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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.

General procedure: To a solution of9(0.16g,0.58mmol) ini-PrOH(5mL),substituted phenylamine(0.64mmol)wasadded. The reaction mixture was stirred at reflux for4h under N2atmosphere. After the reaction was completed, the mixture wasnaturally cooled to room temperature.Themixture was filtered and the solid was collectedto giveintermediate12or15. 1.2.1 (4-((6-Bromoquinazolin-4-yl)amino)phenyl)(4-methylpiperazin-1-yl)methanone (12a)Yellow solid; yield:73 %.MS (ESI)m/z: [M+H]+=426.1/428.1.

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

Reference£º
Article; Xin, Minhang; Hei, Yuan-Yuan; Zhang, Hao; Shen, Ying; Zhang, San-Qi; Bioorganic and Medicinal Chemistry Letters; vol. 27; 9; (2017); p. 1972 – 1977;,
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120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 48.1: 2-(2-Methyl-piperazin-1-yl)-nicotinonitrile. A mixture of 3 -methyl-pip erazine-1-carboxylic acid tert-butyl ester (1.00 g, 5.00 mmol), 2-chloro-nicotinonitrile (1.04 g, 7.48 mmol), triethylamine (2 mL) and tetrahydrofuran (8 mL) was heated at 80¡ã C overnight. The reaction mixture was cooled to room temperature and dichloromethane (300 mL) and aqueous saturated sodium bicarbonate (75 mL) were added. The aqueous mixture was separated and extracted further with dichloromethane (2×150 mL), The combined organic layer was washed with water (150 mL), washed with brine (100 mL), dried over sodium sulfate, filtered and concentrated. The residue was dissolved in dichloromethane (10 mL) and trifluoroacetic acid (10 mL) was added. The reaction mixture was stirred at room temperature for 2.5 hours and then concentrated. The residue was dissolved in 1,2-dichloroethane (5 mL) and the mixture was then concentrated. To the residue was added saturated aqueous sodium bicarbonate (150 mL). The mixture was extracted with dichloromethane (3×100 mL) and the combined organic layer was washed with water (50 mL), washed with brine (50 mL), dried over sodium sulfate, filtered and concentrated. The residue was purified on silica gel using dichloromethane:2M ammonia in methanol (95:5 to 92.5:7) to give 2-(2-methyl-piperazin-l- yl)-nicotinonitrile (48 mg, 5 percent). 1H NMR (300 MHz, CDCl3): delta(ppm) 8.33 (dd, IH), 7.76 (dd, IH), 6.71 (m, IH)3 4.62 (m, IH), 4.03 (bd, IH), 3.35 (m, IH), 3.10 (m, 2H)1 2.90 (m, 2H), 1.75 (bs, IH), 1.34 (d, 3H)., 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2008/112440; (2008); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: To a well-stirred solution of intermediate 5 (2g, 5.6mmol) in C2H5OH(60mL) was added a drop of AcOH. The resulted mixture was refluxed for 0.5h. Then intermediates 8a (2.95g) was added, followed by stirring for 10hat the same temperature. After cooled to room temperature, The resulting solid was collected by filtration and dried to give the target compounds 9a as a light yellow solid in 82% yield.

118753-66-5, As the paragraph descriping shows that 118753-66-5 is playing an increasingly important role.

Reference£º
Article; Wu, Yachuang; Ding, Xiudong; Ding, Liang; Zhang, Yongsheng; Cui, Lei; Sun, Lu; Li, Wei; Wang, Di; Zhao, Yanfang; European Journal of Medicinal Chemistry; vol. 158; (2018); p. 247 – 258;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

630125-91-6, A suspension of 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (247 mg, 0.858 mmol) in DCM (35 mL) was added to a solution of 2-(4-bromo-2-fluorophenyl)acetic acid (200 mg, 0.858 mmol) in DCM (35 mL). HOBt (197 mg, 1.287 mmol), EDC (247 mg, 1.287 mmol) and Et3N (0.359 mL, 2.57 mmol) was added and the mixture was stirred at 26 C. for 3 h. Then the solution was concentrated and distributed between EA and saturated NaHCO3 solution. The combined organic extract was washed with brine, dried over MgSO4, filtered and concentrated. The crude material was purified by silica column chromatography (PE/EA=10/1). All fractions found to contain product by TLC (PE/EA=5/1, Rf=0.6) were combined and concentrated to yield a light yellow solid of 2-(4-bromo-2-fluorophenyl)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)acetamide (413 mg, 0.822 mmol, 96.0% yield): 1H NMR (400 MHz, CD3OD) delta 7.98-7.91 (m, 1H), 7.79-7.67 (m, 2H), 7.40-7.27 (m, 3H), 3.74 (s, 2H), 3.61 (s, 2H), 2.58-2.39 (m, 11H), 1.09 (s, 4H); ES-LCMS m/z 502.0 (M+H).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GlaxoSmithKline Intellectual Property Development Limited; EIDAM, Hilary Schenck; Raha, Kaushik; Gong, Zhen; Guan, Huiping; Wu, Chengde; Yang, Haiying; Yu, Haiyu; Zhang, Zhiliu; CHEUNG, Mui; US2014/275111; (2014); A1;,
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31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(1) 1-Benzyloxycarbonylpiperazine (19.0 g) was dissolved in pyridine (150 mL) and acetic anhydride (9.0 mL) was added at room temperature. The mixture was stirred for 18 hr. The reaction solution was concentrated under reduced pressure, and a 10percent aqueous citric acid solution was added to the residue. The mixture was extracted with ethyl acetate. The extract solution was washed with saturated brine, dried and concentrated under reduced pressure to give 4-acetyl-1-benzyloxycarbonylpiperazine (22.6 g) as an oil.(2) The above-mentioned compound (7.12 g) was dissolved in tetrahydrofuran (150 mL), and a 1 mol/L lithium bis(trimethylsilyl)amide-tetrahydrofuran solution (41 mL) was added dropwise at -78¡ãC over 40 min. After stirring at said temperature for 1 hr, a solution of ethyl trifluoroacetate (4.85 mL) in tetrahydrofuran (20 mL) was added to the reaction solution. The mixture was gradually warmed to room temperature and stirred for 18 hr. A saturated aqueous ammonium chloride solution was added to the reaction solution, and the mixture was extracted with ethyl acetate. The extract solution was washed with saturated brine, dried and concentrated under reduced pressure. The residue was purified by silica gel chromatography to give 1-benzyloxycarbonyl-4-trifluoroacetoacetylpiperazine (7.35 g) as a pale-yellow solid.(3) In the same manner as in Example 36(1) and using the above-mentioned compound (1.96 g) and phenylhydrazine (0.540 mL), 1-benzyloxycarbonyl-4-(3-trifluoromethyl-1-phenyl-5-pyrazolyl)piperazine (0.416 g) was obtained as an oil.(4) In the same manner as in Example 33(3) and using the above-mentioned compound (416 mg), 1-(3-trifluoromethyl-1-phenyl-5-pyrazolyl)piperazine (286 mg) was obtained as a white solid.(5) In the same manner as in Example 29(1) and using the above-mentioned compound (286 mg) and the title compound (280 mg) of Reference Example 3, 3-{(2S,4S)-1-tert-butoxycarbonyl-4-[4-(3-trifluoromethyl-1-phenyl-5-pyrazolyl)-1-piperazinyl]-2-pyrrolizinylcarbonyl}-1,3-thiazolidine (322 mg) was obtained as a pale-brown powder.(6) In the same manner as in Example 33(5) and using the above-mentioned compound (322 mg), the title compound (294 mg) was obtained as a white solid.1H-NMR(DMSO-d6)delta 2.00-2.28(1H,m), 2.80-4.00(16H,m), 4.44-4.74(3H,m), 6.64(1H,s), 7.44-7.49(1H,m), 7.54-7.59(2H,m), 7.77-7.79(2H,m), 9.03(1H,brs), 10.55(1H,brs).

31166-44-6, The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Mitsubishi Pharma Corporation; EP1426366; (2004); A1;,
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630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-(2-(cyclopropanecarboxamido)thiazolo[5,4-b]pyridin-5-yl) benzoic acid (150 mg, 0.44 mmol) and triethylamine (90 muL, 0.66 mmol) in toluene (2 niL) was added diphenylphosphoryl azide (0.11 niL, 0.49 mmol). The resulting mixture was stirred at room temperature for 30 minutes and heated at 80 0C for 1 h. To a reaction mixture was added 4-((4-ethylpiperazin-l-yl)methyl)-3-(trifluoromethyl) aniline (121 mg, 0.42 mmol) and triethylamine (90 muL, 0.66 mmol). The reaction mixture was stirred at 80 0C for 2h and most of organic solvent was removed in vacuo. The crude product was diluted with DMSO (3 mL) and purified by preparative HPLC to give the title compound as a TFA salt.1H NMR 600 MHz (CDCl3) delta 8.51 (s, IH), 7.83 (d, J= 1.8 Hz, IH), 7.48 (m, 2H), 7.19 (m, 3H), 7.12 (m, 2H), 6.85 (J, J= 3.0 Hz, IH), 6.49 (m, IH), 6.19 (m, 2H), 3.84 (m, IH), 3.78 (s, 3H), 3.46 (m, 2H), 3.19 (m, IH), 2.90 (m, 2H), 1.99 (m, 2H), 1.69 (m, 2H), 1.19 (J, J= 6.6 Hz, 6H), MS m/z : 624.36 (M + 1).

630125-91-6, 630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; CHOI, Hwan, Geun; SIM, Taebo; GRAY, Nathanael; ZHOU, Wenjun; CHANG, Jae, Won; ZHANG, Jianming; WEISBERG, Ellen; WO2010/144909; (2010); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

31166-44-6, A mixture of benzyl piperazine-1-carboxylate (Aldrich, 3.19 g, 14.5 mmol), 1-(5-fluoro-2-nitrobenzylsulfonyl)naphthalene (5.00 g, 14.5 mmol), and K2CO3 (4.00 g, 29.0 mmol) in DMF (32 mL) was stirred at 100¡ã C. for 3 hours, cooled to room temperature, diluted with water, and extracted with EtOAc. The organic layer was washed with water (3*), dried over Na2SO4, and concentrated in vacuo to provide the title compound (7.82 g, 94percent), characterized by NMR and mass spectral analyses. MS (ES+) m/e 546 (MH+).

As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Patent; Wyeth; US2009/318470; (2009); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.

5308-25-8, 4.00 g (19.7 mmol) of 5-bromo-2-nitropyridine, 3.40 g (2.98 mmol) of 1-ethylpiperazine, 4.10 g (29.6 mmol) of potassium carbonate, 0.4 g (1.2 mmol) of tetrabutylammonium iodide, and 40mL of DMSO were added to a reaction flask, and reacted at 80C for 16 h. The reaction solution was then poured into ice-water and extracted three times with dichloromethane (20 ml for each time). The organic phases were combined, dried with anhydrous sodium sulfate, filtered, concentrated and separated by column chromatography (DCM/MeOH = 100:1-10:1) to give 3.59 g of yellow solid, yield 56.1%. MS (ESI): m/z 237.2 [M+H]+.

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Gan & Lee Pharmaceuticals; YIN, Lei; LIU, Wenjian; LI, Heng; ZHU, Dianxi; (73 pag.)EP3385262; (2018); A1;,
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