Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of the intermediates 3a-3e (5 mmol) and corresponding secondary amine 4a-4g (5.5 mmol) was added in CH3CN (20 ml) at the presence of anhydrous K2CO3 (6 mmol). The mixture was heated at 65 ¡ãC for 6-10 h. The solvent was evaporated in vacuo. The residue was dissolved in CH2Cl2 (25 mL), washed with water (20 mL ¡Á 3), and the combined organic phases were washed with saturated aqueous NaCl (30 mL), dried over sodium sulfate, and filtered. The solvent was evaporated under reduced pressure. The residue was purified on a silica gel chromatography using mixtures of petroleum/acetone as eluent to get the target products TM-1~TM-28.

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

Reference£º
Article; Sang, Zhipei; Wang, Keren; Wang, Huifang; Yu, Lintao; Wang, Huijuan; Ma, Qianwen; Ye, Mengyao; Han, Xue; Liu, Wenmin; Bioorganic and Medicinal Chemistry Letters; vol. 27; 22; (2017); p. 5053 – 5059;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

A magnetically-stirred 70-mL fluoropolymer-lined steel autoclave was fitted with an internal thermocouple capable of determining the temperature of the liquid phase contained in the vessel, a pressure gauge, a pressure-relief valve, and a vent valve. The amine starting material, anhydrous or aqueous sodium 2-hydroxyethanesulfonate, and anhydrous or aqueous sodium hydroxide were charged to the open autoclave, which was then assembled and immersed in an electrically heated oil bath. With the vent valve closed, the stirred reaction mixture was rapidly heated to the reaction temperature and held at that temperature for the times specified in Examples 9, 10, and 13 below. The reaction mixture was then cooled to ambient temperature, the reactor opened, and the reaction product taken up in sufficient water to dissolve all solids., 103-76-4

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Carroll, Glenn T.; Smith, Gary S.; Stringer, Gary E.; US2006/89509; (2006); A1;,
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20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

20327-23-5, 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 82%, m.p. = 55-57 C (measured),m.p. = 58-60 C (reported) [60]; 4-(4-ethylpiperazin-1-yl)benzaldehyde (1b), CAS No:197638-76-9,Yield 79%, obtained as an oil; 4-(4-isopropylpiperazin-1-yl)benzaldehyde (1c), CAS No:197638-78-1,Yield 84%, obtained as an oil and 4-(4-cylopropylpiperazin-1-yl)benzaldehyde (1d), CAS No:1292778-23-4,Yield 78%, obtained as an oil.

As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

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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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,74879-18-8

Step D: A mixture of 7-fluoro-3-(4-methylthiazol-2-yl)-2H-chromen-2-one (100 mg, 0.38 mmol), (S)-2-methylpiperazine (46 mg, 0.46 mmol) and DMSO (600 muL) was heated at 80 C. for 15 h. The reaction mixture was diluted in an aqueous saturated NaHCO3 solution and filtered. The collected material was purified by silica gel column chromatography (10% MeOH in CH2Cl2), followed by trituration with 1:1 hexane/acetone to yield the title compound (103 mg, 79%) as a yellow solid: m.p. 194-199 C.; MS m/z 342.2 [M+H]+; 1H NMR (500 MHz, DMSO-d6): delta 8.80 (1H, s), 7.75 (1H, d, J=9 Hz), 7.32 (1H, m), 7.06 (1H, dd, J=9 Hz, 2.5 Hz), 6.91 (1H, d, J=2.5 Hz), 3.88 (2H, t, J=11 Hz), 2.96 (1H, d, J=12 Hz), 2.81 (1H, td, J=12 Hz, 3 Hz), 2.72 (2H, m), 2.45 (4H, m), 2.36 (1H, br s), 1.04 (3H, d, J=6.5 Hz).

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PTC Therapeutics, Inc.; F. Hoffmann-La Roche AG; Woll, Matthew G.; Chen, Guangming; Choi, Soongyu; Dakka, Amal; Huang, Song; Karp, Gary Mitchell; Lee, Chang-Sun; Li, Chunshi; Narasimhan, Jana; Naryshkin, Nikolai; Paushkin, Sergey; Qi, Hongyan; Turpoff, Anthony A.; Weetall, Marla L.; Welch, Ellen; Yang, Tianle; Zhang, Nanjing; Zhang, Xiaoyan; Zhao, Xin; Pinard, Emmanuel; Ratni, Hasane; (317 pag.)US9617268; (2017); B2;,
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120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (Q1a) (500 mg, 1.8 mmol, 1 eq), the corresponding cyclic amine (8.9 mmol, 5 eq) and DMSO (3.6 mL) was heated by microwave irradiation at 115 C for 3 h. The resultant mixture was concentrated by freeze drying, and to the residue was added EtOAc (30 mL). The precipitate was isolated by vacuum filtration and washed with EtOAc, water and Et2O to afford the Boc-protected aminated quinolone.

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Lim, Carine S.Q.; Ha, Kam Pou; Clarke, Rebecca S.; Gavin, Leigh-Anne; Cook, Declan T.; Hutton, Jennie A.; Sutherell, Charlotte L.; Edwards, Andrew M.; Evans, Lindsay E.; Tate, Edward W.; Lanyon-Hogg, Thomas; Bioorganic and Medicinal Chemistry; vol. 27; 20; (2019);,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.479353-63-4,1-Boc-4-(4-Carboxybenzyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture of compound 5 (1.0 g, 2.81 mmol), compound 7a (0.98 g, 4.19 mmol), HATU (1.28 g, 3.37mmol) in DMF (20 mL) was cooled to 0C and DIPEA (1.95 mL, 11.24 mmol) was added. The reaction mixture was allowed to warm to room temperature and stirred for 15 min. Saturated aqueous sodium bicarbonate (20 mL) was added and the resulting mixture was extracted with ethyl acetate (50 mL><2). The combined extracts were dried over anhydrous sodium sulfate and concentrated. The residue was purified by flash column chromatography on silica gel (petroleum ether/ethyl acetate = 3 : 1 to 1 : 1) to afford compound 8a (1.29 g, 80% yield) as a yellow solid. 479353-63-4, 479353-63-4 1-Boc-4-(4-Carboxybenzyl)piperazine 2795516, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; INHIBIKASE THERAPEUTICS, INC.; WERNER, Milton, H.; KELLY, Terence, A.; (74 pag.)WO2016/172528; (2016); 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.

4.1.14 (3-Trifluoromethyl-1-phenyl-1H-pyrazol-5-yl)piperazine (12e) To a solution of 10a (19.0 g, 86.3 mmol) in pyridine (150 mL) was added acetic anhydride (9.0 mL, 95 mmol) at room temperature. The mixture was stirred for 18 h, and then concentrated under reduced pressure. The residue was poured into a 10percent aqueous citric acid solution and extracted with ethyl acetate. The extract was washed with brine, dried and concentrated under reduced pressure to give 4-acetyl-1-benzyloxycarbonylpiperazine (22.6 g, 100percent) as an oil. 1H NMR (300 MHz, DMSO-d6): delta 2.78 (2H, s), 3.35-3.68 (8H, m), 5.10 (2H, s), 7.28-7.42 (5H, m).

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

Reference£º
Article; Yoshida, Tomohiro; Akahoshi, Fumihiko; Sakashita, Hiroshi; Kitajima, Hiroshi; Nakamura, Mitsuharu; Sonda, Shuji; Takeuchi, Masahiro; Tanaka, Yoshihito; Ueda, Naoko; Sekiguchi, Sumie; Ishige, Takayuki; Shima, Kyoko; Nabeno, Mika; Abe, Yuji; Anabuki, Jun; Soejima, Aki; Yoshida, Kumiko; Takashina, Yoko; Ishii, Shinichi; Kiuchi, Satoko; Fukuda, Sayaka; Tsutsumiuchi, Reiko; Kosaka, Keigo; Murozono, Takahiro; Nakamaru, Yoshinobu; Utsumi, Hiroyuki; Masutomi, Naoya; Kishida, Hiroyuki; Miyaguchi, Ikuko; Hayashi, Yoshiharu; Bioorganic and Medicinal Chemistry; vol. 20; 19; (2012); p. 5705 – 5719;,
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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.

EXAMPLE 24 9-(2,4-Dichloroanilino)-4-[4-(4-ethyl- 1-piperazinyl)butyl]-3 4-dihydro-2H-[1,4]oxazino[2,3-g]quinoline-8-carbonitrile An amount of 120 mg (0.26 mmol) of 4-(4-chlorobutyl)-9-(2,4-dichloroanilino)-3,4-dihydro-2H-[1,4]oxazino[2,3-g]quinoline-8-carbonitrile was stirred in N,N-dimethylformramide (0.8 mL), and to this were added sodium iodide (55 mg, 0.36 mmol), tetrabutylammonium iodide (58 mg, 0.16 mmol), and 1-ethylpiperazine (0.26 mL, 2.1 mmol). The mixture was heated at 50 C. for three hours, after which an additional amount of 1-ethylpiperazine (0.26 mL, 2.1 mmol), was added. The mixture was heated at 60 C. for 3 hours, and subsequently evaporated to a yellow oil, stirred with saturated sodium bicarbonate solution, and extracted with dichloromethane. The organic layer was washed with saturated brine solution, dried over sodium sulfate, and evaporated to a yellow oil. Purification was performed by flash chromatography (10% acetone in dichloromethane, then 70:30:5=dichloromethane: methanol: ammonium hydroxide), to give a yellow solid (74 mg, 53% yield), m.p 97-98 C.; 1H NMR (DMSO-d6) delta 9.21 (s, 1H), 8.27 (s, 1H), 7.73 (d, 1H), 7.68 (s, 1H), 7.42 (dd, 2H), 6.70 (s, 1H), 4.27 (t, 2H), 3.49 (m, 4H), 2.31 (m, 12H), 1.62 (dd, J=7 Hz, 2H), 1.52 (dd, J=7 Hz, 2H), 0.97 (t, 3H);

5308-25-8, 5308-25-8 1-Ethylpiperazine 79196, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; American Home Products Corporation; US2003/65180; (2003); A1;,
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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

[Referential Example 83]; 3,4-Dimethylpiperazine-1-carboxylic acid tert-butyl ester ; [] 3-Methylpiperazine-1-carboxylic acid tert-butyl ester (5.70 g) obtained from Referential Example 82 was dissolved in methanol (100 mL). To the resultant solution, 10percent palladium-carbon (0.59 g), 35percent aqueous formalin (9.7 mL), and 1M HCl in ethanol (31.3 mL) were added at room temperature, followed by stirring in a hydrogen atmosphere for 15 hours. After the system was purged with nitrogen, insoluble matter was filtered off, and the solvent of the filtrate was evaporated under reduced pressure. To the residue, chloroform – methanol (9percent) was added, and the resultant mixture was alkalinized through addition of aqueous sodium hydroxide, followed by partition. The aqueous layer was extracted with chloroform – methanol (9percent). The organic layers were combined and washed with saturated brine, and then dried over sodium sulfate anhydrate, followed by filtration. The solvent was evaporated under reduced pressure, and the residue was purified through silica gel column chromatography (chloroform – methanol), to thereby give the title compound as an oily product (3.10 g, 51percent).1H-NMR(400MHz,CDCl3)delta: 1.04(3H,d,J=6.3Hz), 1.46(9H,s), 1.95-2.20(2H,m), 2.28(3H,s), 2.50-2.78(2H,br), 2.90-3.05(1H,br), 3.88(1H,br). MS(ESI)m/z: 215(M+H)+.

120737-59-9, Big data shows that 120737-59-9 is playing an increasingly important role.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1591443; (2005); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: The solution of 8 (1 equiv) and substituted phenyl piperazine (1 equiv) in dry DMF (5 ml) was cooled to 0 C. The N-ethyl-N?-(dimethyaminopropyl)carbodimide hydrochloride (EDC¡¤HCl) (1 equiv), 1-hyroxybenzotriazole hydrate (HOBt¡¤H2O) (1 equiv) and DIPEA (2 equiv) were added and the resulting mixture stirred for 24 h at room temperature. H2O (40 ml) was added to reaction mass and extracted with ethylacetate (40 ml ¡Á 3). The combined organic layer was washed with saturated aqueous NaHCO3 solution (30 ml), brine (30 ml), dried over MgSO4 and concentrated to give crude mass which were purified on silica gel CC to afforded desired products 9a-j., 13754-38-6

The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Sharma, Rajni Kant; Younis, Yassir; Mugumbate, Grace; Njoroge, Mathew; Gut, Jiri; Rosenthal, Philip J.; Chibale, Kelly; European Journal of Medicinal Chemistry; vol. 90; (2015); p. 507 – 518;,
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