Heterocyclic Building Blocks-piperazine

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 5; Preparation of Quetiapine from ll-piperazinyldibenzo[b,f][l,4]thiazepine; [0040] 33.1 g of extra fine potassium carbonate is added to the r¡ã-butanol solution of 1 l-piperazinyldibenzo[b,fj[l54]thiazepine with continuous stirring. Then, 16.48 g of sodium iodide and 35.97 g of 2-(2-chloroethoxy)ethanol are respectively added with stirring. With continued mixing, the reaction mixture is heated to a temperature of 102 C and maintained at that temperature for 12 – 16 hours. The conversion of 11- piperazinyldibenzo[b,fj[l,4]thiazepine to quetiapine can be monitored by HPLC analysis. Once the conversion of is complete, the reaction mixture is cooled to a temperature of less than about 80 0C and about 500 g of water is added to adjust the reaction mixture to a temperature of about 40 – 50 C and the mixing is continued for at least about 30 minutes. The biphasic mixture is transferred to a separatory funnel and the aqueous and organic phases are allowed to separate. The lower aqueous phase is isolated and discarded. The upper organic phase containing crude quetiapine is transferred to a flask. Another 25O g of water is added to the quetiapine solution and the reaction mixture is stirred at a temperature of about 40 – 50 C for at least 30 additional minutes. The biphasic mixture is again transferred to a separatory funnel and the aqueous and organic phases are allowed to separate. The lower aqueous phase is removed and discarded. The upper organic phase containing crude quetiapine is recovered and transferred to a flask and distillation setup suitable for vacuum distillation to azeotropically remove water. Vacuum is applied to the distillation setup as the solution is heated, possibly to a temperature as high as 55 – 65 C at the end of the distillation, to remove water. The distillation is continued until no more water is observed collecting in the collection trap. The still bottoms may be checked by KF moisture analysis; the amount of KF water should be less than 0.5% by weight. Once the distillation is complete, the crude quetiapine solution is cooled to a temperature of less than 30 0C., 5747-48-8

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CAMBREX CHARLES CITY, INC.; WO2006/135544; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 10 RRN No.442(R)-tert-Butyl 4-(4-amino-1-methyl-1H-pyrazol-5-yl)-3-methylpiperazine-1-carboxylate [0401] 5-chloro-1-methyl-4-nitro-1H-pyrazole from Example 1 (355 mg, 2.2 mmol) and potassium fluoride (511 mg, 8.8 mmol) in dry DMSO (20 mL) was added (R)-tert-butyl 3-methylpiperazine-1-carboxylate (507 mg, 2.53 mmol) and the mixture was heated in the microwave at 100 C. for 10 hr. The mixture was partitioned between water (40 mL) and EtOAc (100 mL) and the organic layer passed through a phase separation cartridge and concentrated under reduced pressure. Purification via silica gel column chromatography (0-100% EtOAc/isohexane) gave (R)-tert-butyl 3-methyl-4-(1-methyl-4-nitro-1H-pyrazol-5-yl)piperazine-1-carboxylate as an orange gum (627 mg). To a solution of this gum (179 mg, 0.55 mmol) and ammonium formate (256 mg, 4.4 mmol) in MeOH (10 mL) under nitrogen was added 10% palladium on carbon (59 mg, 0.55 mmol). The mixture was heated at 70 C. for 4 hr before being cooled, filtered and concentrated under reduced pressure. The residue was partitioned between water (20 mL) and DCM (60 mL) and the organic layer separated, passed through a phase separation cartridge and concentrated under reduced pressure to give (R)-tert-butyl 4-(4-amino-1-methyl-1H-pyrazol-5-yl)-3-methylpiperazine-1-carboxylate as a brown gum (150 mg, 80% over two steps). LCMS (ES+) m/z 296 (M+1)., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference£º
Patent; GENENTECH, INC.; Hodges, Alastair James; Matteucci, Mizio; Sharpe, Andrew; Sun, Minghua; Wang, Xiaojing; Tsui, Vickie H.; US2013/79321; (2013); A1;,
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Piperazines – an overview | ScienceDirect Topics

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: A suitable commercial phenylpiperazine (2.00-5.10 mmol), K2CO3 (0.9-2.00 g) and acetone (7-16 mL) were stirred and refluxed for 30 min. Then, correspondingly substituted bromopentyl 3-benzyl-5,5-hydantoin derivatives 37-39 (2.20-5.70 mmol) in acetone (9-20 mL) were added and the mixture was refluxed for 6 h, left at room temperature overnight and separated from the inorganic precipitate by filtration. The solvent was evaporated from the filtrate. The pure product (14a-24a) was obtained from the residue using method C or D.

115761-79-0, 115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Handzlik, Jadwiga; Bojarski, Andrzej J.; Sata?a, Grzegorz; Kubacka, Monika; Sadek, Bassem; Ashoor, Abrar; Siwek, Agata; Wi?cek, Ma?gorzata; Kucwaj, Katarzyna; Filipek, Barbara; Kie?-Kononowicz, Katarzyna; European Journal of Medicinal Chemistry; vol. 78; (2014); p. 324 – 339;,
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.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.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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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);,
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.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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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);,
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.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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics