Heterocyclic Building Blocks-piperazine

611225-86-6, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

611225-86-6, 104 mg (0.35 mMol) triphosgene are ^j-n’ ^ dissolved in13 ml ice-cooled CH2CI2. ^-/ ~~” Then a solution of 230 mg (1.05mMol) 4-(4-ethylpiperazin-1-O Hylmethyl)~aniline and 209 i (1.50 mMol) Et3N in 6 ml CH2CI2 is added during 8 min. After 3 additional minutes, the mixture is warmed up to rt by a water bath and then a solution of 1.0 mMol 5-(6-chloro-pyrimidin-4-yioxy)-2,3-dihydro-1H-indole (Step 14.1) and 139 jll. (1.00 mMol) Et3N in 6 ml CH2CI2 is added during 8 min. After 2 h at rt, the mixture is diluted with sat. Na2C03 solution / water 1:1 and EtOAc, the aqueous phase separated off and extracted twice with EtOAc. The organic layers are washed with water and brine, dried (Na2S04) and concentrated. Crystallization from DIPE gives the title compound: MS: [M+1]+= 493 / 495; TLC(CH2CI2/MeOH/NH3conc- 90:10:1): Rf = 0.24; HPLC: et_ = 10.5.

The synthetic route of 611225-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2006/34833; (2006); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

General procedure: A solution of compound 4 or 5 (1 mmol) and the appropriate aniline (1 mmol) in n-butanol (5 mL) was stirred at 100 C for 5 h. The reaction mixture was then cooled to room temperature, evaporated under reduced pressure, and the residue was purified either by flash column chromatography or precipitation., 115619-01-7

As the paragraph descriping shows that 115619-01-7 is playing an increasingly important role.

Reference：
Article; Elkamhawy, Ahmed; Al-Sanea, Mohammad M.; Song, Chiman; Sim, Taebo; Roh, Eun Joo; Bulletin of the Korean Chemical Society; vol. 36; 7; (2015); p. 1863 – 1873;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

Step-2: To a solution of (E)-methyl 1-acetyl-3-(ethoxy(phenyl)methylene)-2-oxo-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine-6-carboxylate (2.6 g, 7.10 mmol) in DMF (5 mL) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (1.94 g, 7.43 mmol) at RT and the reaction mixture was heated to 110 C. and stirred for 1 h. The reaction mixture was allowed to cool to RT, treated with piperidine (3 mL) and stirred for 30 min. The reaction mixture was evaporated and the resultant residue was purified by silica gel column chromatography using 5% CH3OH in dichloromethane as eluent to afford (Z)-methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxo-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine-6-carboxylate as yellow solid. MS (ES+): m/z 541.1 (MH+).

262368-30-9, As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference：
Patent; ANGION BIOMEDICA CORP.; PANICKER, Bijoy; MISHRA, Rama K.; LIM, Dong Sung; OEHLEN, Lambertus J.W.M.; JUNG, Dawoon; US2015/306078; (2015); A1;,
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115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Additional amide analogs were prepared by adding 1.5 equivalents of an amine which will provide the desired substituents into a 1 dram vial (1.5 eq.) along with lithium 5-amino-7- methoxyimidazo[1,2-c]quinazoline-2-carboxylate (30 mg, 0.114 mmol) and a DMF solution (1.0 ml) solution of DIPEA (0.079 ml, 0.454 mmol), shaking the vial for 5 minutes in a Bohdan Miniblock Shaker and then adding 1-propanephosphonic acid cyclic anhydride (50% w/w in EtOAc, 64.7 mul, 0.109 mmol), and continuing to shake the vial at RT overnight. The completed reaction was quenched with 1.0 ml water and the organic layer separated by filtering through a Varian 2 ml Reservior Frit and a Whatman 0.45mum syringe filter to remove emulsion, followed by solvent removal using a Genevac. The crude residue was dissolved in 1.0 ml DMSO and purified by LC/MS.

115761-79-0, The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; ALI, Amjad; LIM, Yeon-Hee; GALLO-ETIENNE, Gioconda, V.; KELLY, Joseph, Michael; BERLIN, Michael; TING, Pauline; TAGAT, Jayaram, R.; XIAO, Dong; KUANG, Rongze; WU, Heping; WANG, Hongwu; (157 pag.)WO2019/118313; (2019); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

General procedure: To a solution of triphenylphosphine (0.37 mmol) in THF (30 mL) was slowly added diisopropyl azodicarboxylate (0.37 mmol) in 15 min at 0 C and the mixture was stirred for another 15 min. At the same temperature, to the resulting mixture was slowly added a solution of 20 (0.185 mmol) and corresponding alcohol (0.37 mmol) dissolved in 20 mL THF. The ice bar was removed and the reaction mixture was stirred at room temperature for 12 h. The reaction mixture was evaporated in vacuo, and the residue was purified by column chromatography to afford the product., 5317-33-9

5317-33-9 3-(4-Methylpiperazin-1-yl)propan-1-ol 79208, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Xing, Weiqiang; Ai, Jing; Jin, Shiyu; Shi, Zhangxing; Peng, Xia; Wang, Lang; Ji, Yinchun; Lu, Dong; Liu, Yang; Geng, Meiyu; Hu, Youhong; European Journal of Medicinal Chemistry; vol. 95; (2015); p. 302 – 312;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, Di-tert-butyl dicarbonate (3.92 g, 17.98 mmol) was added to a suspension of 2-piperazinone (1.50 g, 14.98 mmol) in dichloromethane (15 mL). The mixture was stirred at room temperature for 5 hours. The solvent was evaporated to afford 1 ,1- dimethylethyl 3-oxo-1-piperazinecarboxylate (2.99 g, quantitative) as an off-white solid.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; PEAT, Andrew, James; PRICE, Daniel, J.; SHOTWELL, John, Brad; TAI, Vincent; ZHANG, Huichang; WO2011/41713; (2011); A2;,
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.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, Example 69 Preparation of ethyl6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate To a stirred solution of 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzeneamine (30.6 mg) in 1,4-dioxane (1 Ml), was added 4-nitrophenylchloroformate (21.6 mg) at room temperature. After 60 C. at 1 h, them mixture was cooled to rt and ethyl 6-(3-aminophenyl)-1H-indazole-3-carboxylate (30 mg) was added. The mixture was stirred at 90 C. for 12 h. Ethyl acetate and water were added and the aqueous layer was extracted with ethyl acetate three times. The combined organic layer was dried over magnesium sulfate and concentrated under reduced pressure. The residue was triturated in ethyl acetate/hexane to give 6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate (16.2 mg). 1H NMR (400 MHz, DMSO-d6) delta13.98 (s, 1H), 9.09 (s, 1H), 8.93 (s, 1H), 8.15 (8.4 Hz, 1H), 7.99 (s, 1H), 7.93 (s, 1H), 7.81 (s, 1H), 7.62 (m, 3H), 7.43 (br d, J=4.4 Hz, 2H), 7.28 (m, 1H), 4.41 (q, J=7.2 Hz, 2H), 3.54 (s, 2H), 2.49 (m, 10H), 1.39 (t, J=7.2 Hz, 3H).

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

Reference：
Patent; Sim, Tae Bo; Son, Jung Beom; Kim, Hwan; Park, Dong Sik; Choi, Hwan Geun; Ham, Young Jin; Hah, Jung Mi; Yoo, Kyung Ho; Oh, Chang Hyun; Lee, So Ha; Ha, Jae Du; Cho, Sung Yun; Kwon, Byoung Mog; Han, Dong Cho; US2012/130069; (2012); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.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,as a common compound, the synthetic route is as follows.

Synthesis of 6-Ffuoro-7-{4-[5-hydroxy-6-(2-methyl-5-nitro- imidazoi-I-yi)-hexyl]-piperazin-I-yi}-l -methyS-4-oxo-4H-2-thia-8b-aza- cyclobu a[a]naphthaSene-3-carboxylic acid (1 15): To a stin-ed solution of 6- Fluoro- 1 -methy-4-oxQ-7-piperazin- 1 -yl-4H-2-thia-8P-aza- cyclobuta[a]naphthalene-3-carboxylic acid, (HI) ( 1 .10 g, 3.16 mmol) in dimethylformamide (30ml) was added potassium carbonate (0.43g, 3.16 mmol) followed by addition of compound (II) (0.85g, 2.63 mmol) and the reaction 1 26 mixture was stirred at RT for 1 6h. The reaction mixture was diluted with ethyl acetate, washed twice with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while euting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (115) with 20% isolated yield. 1 H-NMR (400 MHz, DMSO) delta ppm: 1 .61 – 1 -68(6H, m, CH2), 2.1 (3H, d, J = 6 Hz, CH3), 2.44 (3H, s, CH3) , 2.54 (4H, m, 2 xCH2), 3.2 (4H, m, 2 xCH2), 3.9-4. 1 (2H. m, 2 x CH2N), 4.38( 1 H, d, J = 14, CHOH). 5.2 1 1 H, d, J = 4.4, OH), 6.38 ( 1 H, d, J = 5.6Hz, CHSN) 6.9 ( 1 H, d, J = 6.8, Ar-H). 7.78 ( 1 H, d, J = 1 4 Hz, Ar-H). 8.02 ( 1 H, s, Ar-H). ESI-MS (m/z): 575(M+H)

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
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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

3-METHYLPIPERAZINE-1-CARBOXYLIC acid test-butyl ester (160 mg; 0.80 MMOL ; 2 eq.) (prepared as reported in J. Med. Chem. 1993,36, 690-698), cesium carbonate (195 mg; 0.6 MMOL ; 1.5 eq. ), palladium acetate (9 mg; 0.04 MMOL ; 0.10 eq. ) and 2,2′- bis (diphenylphosphino)-1, 1′-binaphthyl (38 mg; 0.06 MMOL ; 0.15 eq. ) were added to a solution of 2-METHYLQUINOLIN-5-YL-TRIFLUOROMETHANESULFONATE (D1) (117 mg, 0.4 MMOL ; 1 eq) in dry toluene (2.5 mL) under nitrogen. The reaction mixture was stirred at reflux under nitrogen for 10 h. The reaction was cooled and filtered through a pad of celite which was then washed with DCM (50 mL). The filtrates was concentrated in vacuo and the crude product was purified by SPE cartridge (Si, 2g), eluting with 5percent ethylacetate in cyclohexane to afford 3-methyl-4-(2-methylquinolin-5-yl)piperazin-1- carboxylic acid tert-butyl ester as a yellow oil (84 mg; yield 62percent). MS; (ES) m/z: 341.45 [MH] +. C2OH27N302 requires 342. 4.APOS;H-NMR (300 MHz, CDCI3) 8 : 8.5 (d, 1H), 7.77 (d, 1 H), 7.61 (t, 1 H), 7.29 (d, 1 H), 7.12 (d, 1 H), 3.8-3. 6, m/m, 2H), 3. 4- 3. 3 (m, 1 H), 3. 2- 3. 1 (m, 1 H), 3.1-2. 9 (m, 2H), 2.74 (s, 3 H), 1.45 (s, 9H), 1.36 (d, 3H). This compound (84 mg) was dissolved in a mixture 3: 1 of trifluoroacetic acid: DCM (4 mL) and stirred at r. T. for 6h. The solvent was evaporated in vacuo and the residue purified on SCX cartridge (1G) to afford the title compound (D14) (44 mg; yield 76percent) MS; (ES) m/z: 241.45 [MH] +. C15H19N3 requires 242.4. 1H-NMR (300 MHz, CDCI3) 8 : 8.5 (d, 1H), 7.77 (d, 1 H), 7.61 (t, 1 H), 7.29 (d, 1 H), 7.12 (d, 1 H), 3.3 (m, 4H), 3.15 (m, 4 H), 2.74 (s, 3 H), 1.9 (m, 2H)., 120737-59-9

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

Reference：
Patent; GLAXO GROUP LIMITED; WO2004/46124; (2004); A1;,
Piperazine – Wikipedia
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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.

A mixture of acetoxymethyl 4-nitrophenyl carbonate (1 mmol) and PDBTZ (1 mmol) in hexamethylphosphoramide (1.3 mL) is stirred at ambient temperature until complete by thin layer chromatography. The mixture is diluted with water (35 mL) and extracted with diethyl ether. The extract is washed (aqueous sodium hydroxide, water), dried (sodium sulfate), evaporated, and purified by flash chromatography to provide title compound., 5747-48-8

Big data shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2008/79839; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics