Heterocyclic Building Blocks-piperazine

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

7-Bromo-1H-indole-2-carboxylic acid (1) (2.4 g, 10 mmol), 4-((4-methylpiperazin-1-)methyl)-3-(trifluoromethyl)aniline(2.73g, 10mmol) and 2-(7-oxobenzotriazole)-N,N,N’,N’-tetramethyluronium hexafluorophosphate (HATU)(3.8 g, 10 mmol) dissolved in N,N-dimethylformamide,Diethylisopropylamine (1.65 mL, 10 mmol) was added.Stir until the reaction is complete, extract with ethyl acetate and water,The organic phase was concentrated and subjected to column chromatography to give 3.5 g of product, yield 70%., 694499-26-8

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Beijing Seth Ming Qiang Pharmaceutical Technology Co., Ltd.; Zhang Qiang; Zhang Hongbo; Zhou Likai; Feng Shouye; Yang Hailong; Wang Zhongxiang; (54 pag.)CN109988151; (2019); A;,
Piperazine – Wikipedia
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630125-91-6,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.

To a suspension of triphosgene (0.21 g, 0.71 mmol) and Na2C03 (0.45 g, 4.27 mmol) in DCM (18 ml), kept at 0 ocunder argon, 4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (0.61 g, 2.13 mmol) was added. Thereaction was monitored by HPLC (following the formation of 4-ethyl-piperazine-1-carboxylic acid [4-(4-ethylpiperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-amide by treating a sample of the reaction mixture with N-25 ethylpiperazine). After 1 h, 3-ethynyl-phenylamine (0.26 g, 2.18 mmol) was added and the reaction was let understirring overnight at r.t.. The mixture was diluted with DCM, washed with water (3 x 10 ml), dried over anhydrousNa2S04 and concentrated under vacuum. Purification by flash column chromatography (DCM/MeOH 95/5) affordedthe product as yellow solid (0.64 g, 70%).1H NMR (600 MHz, DMSO-dG) o ppm 0.95-1.00 (m, 3 H) 2.22-2.47 (m, 10 H) 3.52 (s, 2 H) 4.14 (s, 1 H) 7.09 (d,30 J=7.69 Hz, 1 H) 7.30 (t, J=7.88 Hz, 1 H) 7.41 (dd, J=8.24, 1.28 Hz, 1 H) 7.56 (dd, J=8.61, 1.83 Hz, 1 H) 7.61 – 7.64(m, 1 H) 7.66 (t, J=1.65 Hz, 1 H) 7.95 (d, J=2.01 Hz, 1 H) 8.85 (s, 1 H) 9.02 (s, 1 H).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference：
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; MENICHINCHERI, Maria; ANGIOLINI, Mauro; BERTRAND, Jay Aaron; CARUSO, Michele; POLUCCI, Paolo; QUARTIERI, Francesca; SALOM, Barbara; SALSA, Matteo; ZUCCOTTO, Fabio; WO2014/72220; (2014); 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.187669-60-9,1-(4-(Methylsulfonyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 77; 4-{2-[4-(4-Methanesulfonylphenyl)piperazin-l-yl]ethylidene}piperidine-l- carboxylic acid tert-butyl ester; To a solution of 4-(2-hydroxyethylidene)piperidine-l-carboxylic acid tert-butyl ester (2.2g, 9.7mmol) in DCM (25mL) was added Et3N (2.02mL, 14.5mmol) and the reaction cooled to O0C. To this cooled mixture was added methanesulfonylchloride (0.98mL, 12.6mmol) dropwise. The reaction was stirred at O0C for 20 min then treated with saturated NaHCO3 solution. The two layers were separated and the organic layer washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by flash chromatography with 10% EtOAc / Hexane as eluent to afford 4-(2-chloroethylidene) piperidine-1-carboxylic acid tert-butyl ester and 4-vinyl-3,6-dihydro-2H-pyridine-l-carboxylic acid tert-butyl ester in a 1:1 ratio (0.95Og). The mixture was dissolved in DMF (5mL) and treated with TBAI (0.068g, 0.18mmol). This suspension was thus added to a preformed mixture of l-(4-methanesulfonylphenyl)piperazine (0.487g, 2.03mmol) and sodium hydride (0.1 Ig of a 60% dispersion in mineral oil, 2.77mmol) in DMF (5mL) at rt. The mixture was allowed to stir for 2h then treated with water. The aqueous was extracted with EtOAc and the combined organic layers washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by HPLC to afford the title compound (0.27g, 6%): RT = 2.41 min; m/z (ES+) = 450.2 [M+ H]+, 187669-60-9

As the paragraph descriping shows that 187669-60-9 is playing an increasingly important role.

Reference：
Patent; PROSIDION LIMITED; WO2007/3964; (2007); 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.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

5271-27-2, 24. (2,4-bis(allyloxy)-5-isopropylphenyl)(4-methyl-2-phenylpiperazin-1-yl)methanone (16) Compound 14 (0.18 g, 0.66 mmol), 1-methyl-3-phenylpiperazine (0.18 g, 0.99 mmol), 1-ethyl-3-(3-dimethylaminopropyl) (0.25 g, 1.33 mmol), 1-hydroxybenzotriazole (0.09 g, 0.66 mmol) and N,N-diisopropylethylamine (0.09 mL, 0.66 mmol) were dissolved in 4 ml of DMF and stirred at 120° C. for 3 hours under a microwave irradiation (Biotage Initiator). The reaction mixture was diluted with ethyl acetate and the organic layer was washed with 1 N HCl solution. It was dried over Na2SO4, concentrated under pressure and purified by MPLC to obtain Compound 16 in a yield of 92percent. Rf=0.24 (3:7 ethyl acetate:hexane).

The synthetic route of 5271-27-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; INDUSTRY ACADEMIC COOPERATION FOUNDATION KEIMYUNG UNIVERSITY; SEO, Young Ho; (32 pag.)US2019/31620; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

848482-93-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.848482-93-9,(S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

(S)-4-Boc-2-piperazinecarboxylic acid (530 mg, 2.17 mmol) was dissolved in MeOH (25 mL) and formaldehyde (1.76 mL, 37 wt % in water, 21.7 mmol) was added. The reaction mixture was stirred for 30 min, NaBH(OAc)3 (0.92 g, 4.34 mmol) was added and the reaction mixture was stirred for 2 h. The solvents were removed in vacuo and the residue was purified by reverse phase column chromatography. The residue and benzyl homopiperazine (0.41 g, 2.17 mmol) were dissolved in DMF (20 mL) and cooled to 0 C. DIPEA (0.59 g, 4.56 mmol) and HBTU (0.82 g, 2.17 mmol) were added and the reaction mixture was stirred for 3 h. The solvents were removed in vacuo and the residue was partitioned between DCM (100 mL) and water (50 mL). The organic fraction was washed with 1M aq Na2CO3 (25 mL), brine (25 mL), dried (MgSO4) and concentrated in vacuo. The residue was purified by reverse phase column chromatography to give the title compound (0.64 g, 71%) as a light yellow gum. LCMS (ES+): 417.4 [MH]+.

The synthetic route of 848482-93-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Proximagen Limited; Savory, Edward Daniel; Stewart, Allson; Cartey, Allison; Brown, Giles; Simpson, Iain; Oliver, Kathryn; Patient, Lee; Higginbottom, Michael; Cole, Andrew Graham; US2013/289020; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

2759-28-6, 1-Benzylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Amine (1 mmol) and di-tert-butyl dicarbonate [(Boc)2O] (1.1 mmol) were placed in a microwave reaction vial. The LG microwave oven MG 555f was programmed to 300 W at 100 C. The reaction was monitored using TLC. After the reaction, ice water was added to the reaction mixture which resulted in the precipitation of the product. The solid product was merely filtered off and washed with excess cold water. The product was pure enough for all practical purposes. For characterization purpose, it was further purified by column chromatography (Neutral Alumina as adsorbent, solvent system: Hexane: Ethyl acetate (7.5:2.5)).

2759-28-6, The synthetic route of 2759-28-6 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Dighe, Satish N.; Jadhav, Hemant R.; Tetrahedron Letters; vol. 53; 43; (2012); p. 5803 – 5806;,
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

A mixture of 2-(3-bromo-5-fluoro-phenyl)-3,3-dimethyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid methyl ester (0.41 g, 1.0 mmol), 1-isopropyl piperazine (0.64 g, 5.0 mmol), copper (I) iodidie (120 mg, 0.6 mmol), L-proline (69 mg, 0.6 mmol) and potassium hydroxide (33.6 mg, 0.6 mmol) in DMSO (2 mL) was stirred at 120° C. for 2 hours. Then treated with saturated ammonium chloride (20 mL), extracted with ether (100 mL). After removal of solvent, the residue was purified on flash silica gel chromatography (silica gel from QingDao, 200-300 mesh, glass column from Shanghai SD company) (40percent ethyl acetate/hexanes) to afford 2-[3-fluoro-5-(4-isopropyl-piperazin-1-yl)-phenyl]-3,3-dimethyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid ethyl ester (0.27 g, 60percent) as a white solid: LC/MS m/e calcd for C27H36FN3O2 (M+H)+: 454.6, observed: 454.3

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

Reference：
Patent; Chen, Li; Feng, Lichun; Huang, Mengwei; Liu, Yongfu; Wu, Guolong; Wu, Jim Zhen; Zhou, Mingwei; US2011/257151; (2011); 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.1235865-77-6,2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

(0122) To a mixture of Compound 3J (59.8 mg, 0.105 mmol), Compound 11B (33 mg, 0.105 mmol) and N,N-dimethylpyridin-4-amine (38.4 mg, 0.314 mmol) in dichloromethane (5 ml) was added 1-ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (24.07 mg, 0.13 mmol). The reaction mixture was stirred at room temperature overnight and concentrated. The residue was purified by reverse phase HPLC on a C18 column using a gradient of 40-60% acetonitrile/0.1% trifluoroacetic acid in water to give the title compound as the trifluoroacetate salt. The trifluoroacetic acid salt was dissolved in dichloromethane (6 ml) and washed with 50% aqueous NaHCO3. The organic layer was dried over anhydrous Na2SO4 and concentrated to give the title compound. 1H NMR (500 MHz, dimethylsulfoxide-d6) delta 11.68 (s, 1 H), 11.40 (s, br, 1 H), 8.53-8.58 (m, 2 H), 8.04 (d, 1 H), 7.80 (dd, 1 H), 7.47-7.54 (m, 3 H), 7.34 (d, 2 H), 7.02-7.09 (m, 3 H), 6.67 (dd, 1 H), 6.39 (dd, 1 H), 6.19 (d, 1 H), 3.79 (dd, 1 H), 3.69-3.73 (m, 1 H), 3.22-3.37 (m, 3 H), 3.16-3.21 (m, 1 H), 3.07 (s, 4 H), 2.74 (s, 2 H), 2.09-2.24 (m, 6 H), 1.95 (s, 2 H), 1.86-1.93 (m, 1 H), 1.79-1.85 (m, 1 H), 1.58-1.64 (m, 1 H), 1.42-1.51 (m, 1 H), 1.38 (t, 2 H), 1.25-1.34 (m, 1 H), 0.92 (s, 6 H).

1235865-77-6, As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference：
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

303-26-4, 1-((4-Chlorophenyl)(phenyl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1 : Preparation of5-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-l-yl)-N-(4-methylbenzyl)-3-meth yl-5-oxopentanamide; [147] [148] 0.5 mmol of 4-(4-methylbenzylcarbamoyl)-3-methylbutanoic acid prepared inPreparative Example 1, 0.55 mmol of l-(4-chlorobenzhydryl)piperazine, and ben- zotriazol-1-yloxytripyrrolidino phosphonium hexafluorophosphate (PyBOP) were added to 3 mL of dimethylformamide (DMF) to dissolve. Then, 1.0 mmol of N,N-diisopropylethylamine (DIEA) was added thereto, and stirred at room temperature for 16 hours. 20 mL of 10% HCl was put into the reaction solution, and extracted with 30 mL of EtOAc. The organic layer was washed with 20 mL of 10% HCl, and then washed with 20 mL of a saturated NaHCO solution twice and with 20 mL of a saturated NaCl solution twice. The organic layer was collected, dried over anhydrous MgSO 4 , and filtered under reduced pressure. The organic solvent in the filtrate was removed under reduced pressure. The residue was purified by column chromatography with a mixed solvent of EtOAc and methanol (20:1), so as to obtain the title compound (light yellow solid, yield: 65%).[149] mp 62-630C;[150] 1U NMR (CDCl ) delta 7.35 (d, J=8.0 Hz, 2CH), 7.29 (d, J=7.2 Hz, 2CH), 7.26 (t, J=8.2 Hz, 2CH), 7.22 (t, J=7.3 Hz, CH), 7.16 (d, J=8.0 Hz, 2CH), 7.11 (d, J=7.2 Hz, 2CH), 6.29 (s, NH), 4.37 (d, J=5.6 Hz, CH2), 4.21 (s, CH), 3.59 (t, J=5.6 Hz, CH2), 3.48 (q, J=5.6 Hz, CH2), 2.43 (d, J=6.8 Hz, CH2), 2.34-2.39 (m, CH2), 2.32 (s, CH3), 2.28 (d, J=6.0 Hz, CH ), 2.25 (d, J=6.4 Hz, CH ), 2.13-2.23 (m, CH), 1.03 (d, J=6.4 Hz, CH3);[151] HR-FABMS Calcd for C H ClN O : (M++l): 518.2574, Found: 518.2584.31 36 3 2

303-26-4, As the paragraph descriping shows that 303-26-4 is playing an increasingly important role.

Reference：
Patent; PARK CHOO, Hea-Young; WO2007/142431; (2007); A1;,
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

cis-3,5-Dimethyl-1-(4-trifluoromethoxy-benzyl)-piperazine: To a solution of 4-(trifluoromethoxy)-benzaldehyde (776 uL, 4.38 mmol) in methylene chloride (30 mL) was added cis-2,6-dimethyl piperazine (1.0 g, 8.77 mmol). After 1 hour sodium triacetoxy borohydride (2.45 g, 8.77 mmol) was added to the mixture. The solution was stirred at room temperature for an additional 4 hours. The reaction was concentrated in vacuo, diluted with ethyl acetate and extracted with 1N HCl (2.x.50 mL). The aqueous layer was then neutralized with NaOH and extracted with ethyl acetate (3.x.50 mL). The organic layer was dried (Na2SO4) and concentrated to provide cis-3,5-dimethyl-1-(4-trifluoromethoxy-benzyl)-piperazine (1.01 g, 80percent). 1H NMR (400 MHz, CD3OD) delta 7.42 (d, 2H), 7.23 (d, 2H), 3.54 (s, 2H), 2.98-2.88 (m, 2H), 2.82-2.74 (m, 2H), 1.69 (t, 2H), 1.05 (d, 6H); LCMS 289.5 (M+1)+.

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

Reference：
Patent; KALYPSYS, INC.; US2008/4281; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics