Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of 214 mg (1 mmol) tert-butyl (2S,5R)-2,5-dimethylpiperazine-1 – carboxylatein 3.3ml THF were added at RT 1.74 mL DIPEA (10 mmol, 10 eq) and 176 mg benzenesulfonyl chloride (1 mmol, 1 eq) and the mixture was stirred for 3 days at RT. The mixture was evaporated to yield 440 mg (124%) of the crude title compound which was used in the next step without further purification. LC-MS (Method 1 ): Rt = 1 .30 min; MS (ESIpos): m/z = 355 [M+H]+ (0524) 1H-NMR (500 MHz, DMSO-d6) delta [ppm]: 0.81 (3H), 0.99 (3H), 1 .37 (9H), 3.08 – 3.19 (3H), 3.51 – 3.67 (3H), 4.00 – 4.34 (2H), 7.62 (2H), 7.69 (1 H), 7.79 (2H).

548762-66-9, The synthetic route of 548762-66-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; KOPPITZ, Marcus; SIEBENEICHER, Holger; STEUBER, Holger; TER LAAK, Antonius; NUBBEMEYER, Reinhard; ROTTMANN, Antje; IRLBACHER, Horst; BADER, Benjamin; PETERS, Michaele; WAGENFELD, Andrea; (157 pag.)WO2018/114670; (2018); 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.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

A solution of 4-(2,4-dichloro-phenyl)-1H-pyrazole-3-carboxylic acid (70 mg; 0.27 mmol), 4-(4-methyl-piperazin- 1-yl)-benzylamine (62 mg; 0.3 mmol), EDAC (63 mg; 0.33 mmol) and HOBt (45 mg; 0.33 mmol) in 5 ml of DMF was stirred at room temperature for 48 hours. The reaction was evaporated and the residue partitioned between ethyl acetate and brine. The ethyl acetate layer was separated, dried (MgSO4), filtered, evaporated then dried further under vacuum to give 34 mg of 4-(2,4-dichloro-phenyl)-1H-pyrazole-3-carboxylic acid 4-(4- methyl-piperazin-1-yl)-benzylamide. (LC/MS: Rt 2.42 [M+H]+444).

216144-45-5, The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; WO2006/77424; (2006); A1;; ; Patent; ASTEX THERAPEUTICS LIMITED; WO2006/77428; (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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a solution of 53 7-bromo-4,6-dichloro-3-nitroquinoline (2.07 g, 6.43 mmol) in 78 THF (50 ml) was added 242 1-(tert-butyl) 3-methyl piperazine-1,3-dicarboxylate (2.356 g, 9.64 mmol) followed by 56 DIPEA (3.36 ml, 19.29 mmol) under nitrogen. The reaction was then heated at reflux overnight, cooled and evaporated, taken up in water and extracted with DCM then dried by passing through a phase separator cartridge. Evaporation afforded an orange gum which was purified by flash silica chromatography, elution gradient 0 to 50% 57 EtOAc in 58 heptane. Pure fractions were evaporated to dryness to afford 243 1-(tert-butyl) 3-methyl-4-(7-bromo-6-chloro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (1.66 g, 49%) as a yellow foam. 1H NMR (400 MHz, DMSO, 30 C.) 1.45 (9H, s), 3.30 (1H, s), 3.55 (3H, s), 3.59-3.69 (1H, m), 3.72 (1H, d), 3.75 (1H, d), 3.84 (1H, s), 4.11 (1H, s), 4.35 (1H, s), 8.50 (1H, s), 8.54 (1H, s), 9.12 (1H, s). m/z: ES+ [M+H]+ 529., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

76003-29-7, The N – Boc – 3 – oxo-piperazine (1 g, 5 mmol) is added in the three-necked bottle, adding anhydrous DMF (25 ml), under the protection of argon, adding NaH (300 mg, 7.5 mmol), 25 C stirring 60 min after, dropwise added bromoethane (0.45 ml, 6 mmol), reaction at room temperature overnight. The next day to stop reaction, water, ethyl acetate (50 ml ¡Á 2) extraction, the combined organic layer, saturated NaCl (25 ml ¡Á 2) washing, water-free magnesium sulfate drying, column chromatography (D: M=100:1), shall be the oil of 900 mg, yield 78.9%.

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; Chinese Academy Of Medical Sciences Pharmaceutical Institute; Xu Boling; Chen Xiaoguang; Zhou Jie; Ji Ming; Yao Haiping; Zhou Qin; (57 pag.)CN107098886; (2017); A;,
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108-49-6, 2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The 2,6-dimethyl piperazine dissolved in about 20 ml anhydrous DCM, 0 C Boc anhydride is added dropwise under anhydrous DCM solution, 0 C to continue reaction 1h, water washing, concentration, silica gel column chromatography to 702 mg yellow oily, yield 74.8%., 108-49-6

As the paragraph descriping shows that 108-49-6 is playing an increasingly important role.

Reference£º
Patent; Institute Of Materia Medica Chinese Academy Of Medical Sciences; Xu, Bailing; Chen, Xiaoguang; Yao, Haiping; Ji, Ming; Jin, Jing; Zhou, Jie; Wang, Ke; Zhao, Dalong; (55 pag.)CN105461697; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8,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) 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine. 11-Piperazinyldibenzo[b,f][1,4]thiazepine (0.1 mole), sodium carbonate (0.18 mole), sodium iodide (0.016 mole) and 2-chloroethoxyethanol (0.108 mole) were combined together in toluene (250 ml) and N-methylpyrrolidone (55 ml). The reaction was heated at reflux over 24 hours. The reaction was cooled and washed with water (1 * 175 ml., 2 * 60 ml.). The organic phase was dried by azeotropic distillation. A solution of fumaric acid (0.06 mole) in ethanol (110 ml) was added to the toluene solution at 60-70C. On cooling the hemifumarate salt crystallized out and was isolated by filtration in 75% yield, m.pt 172-173C.

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; IMPERIAL CHEMICAL INDUSTRIES PLC; EP282236; (1988); 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

General procedure: In a dry sealed tube under argon were placed, to a solution of 1-Boc-piperazine (5.04 mmol), potassium carbonate (13.1 mmol) in acetonitrile (12.6 mL) was added 2,5-dibromo pyrimidine13(5.04 mmol). The mixture was allowed to stir at 80 C for 12 h. After completion of the reaction (monitored by TLC), the mixture was then cooled at room temperature, then it was quenched with saturated aqueous NH4Cl (10 mL) and extracted with EtOAc. The organic layers were dried over anhydrous MgSO4and concentrated in vacuo. The resulting residue was purified by flash column chromatography on silica gel (EtOAc:n-hexane = 1:8) to afford piperazine11a., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Kim, Juhyeon; Kim, Yoon Jung; Londhe, Ashwini M.; Pae, Ae Nim; Choo, Hyunah; Kim, Hak Joong; Min, Sun-Joon; Molecules; vol. 24; 18; (2019);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1-piperazin-1-ylethanone (2.00 g, 15.6 mmol) and K 2CO 3 (4.31 g, 31.2 mmol) in CH 3CN (50.0 mL) was added 3-bromopropan-1-ol (3.25 g, 23.4 mmol). The mixture was stirred at 80¡ã C. for 5 hours. The solid was filtered and the filtrate was evaporated to give 1-[4-(3-hydroxypropyl)piperazin-1-yl]ethanone (2.00 g, 10.7 mmol, 68.8% yield) as a colorless oil., 13889-98-0

13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Mirati Therapeutics, Inc.; Array BioPharma Inc.; Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E.; US2019/144444; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5464-12-0,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

4-Nitrophenyl chloroformate (9.85 g, 49 mmol) was dissolved in DCM (200 mL), and cooled to 0¡ã C. 2-(4-methylpiperazin-1-yl)ethanol from the previous step (7.2 g, 50 mmol) and NMM (6 mL) were added, and the reaction mixture allowed to warm gradually to room temperature over 16 hours. The reaction mixture was washed with 1M aq Na2CO3 solution. The organic phase was dried (MgSO4), filtered and concentrated in vacuo to give 2-(4-methylpiperazin-1-yl)ethyl 4-nitrophenyl carbonate (10.7 g, 71percent) as a yellow oil which solidified on standing.Analytical LCMS: purity 80percent (System B, RT=1.70 min), ES+: 310.4 [MH]+.

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; Biovitrum AB; US2009/203695; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

630125-91-6, A mixture of the product of Step C (49 mg, 0.17 mmol) and Intermediate 1(50mg, 0.14 mmol) in 1,4-dioxane (2 mL) was stirred at 100C under N2 for 2 hours (monitored by LCMS).The resulting solution was concentrated under reduced pressure and purified by prep-HPLC to get the title compound (20 mg, 23%) as a white solid. ?H NMR (400 IVIFIz, DMSO-d6) 10.44 (s, 1H), 8.86 (s, 1H), 7.92 (d, J= 5.6 Hz, 1H), 7.90 (d, J= 1.6 Hz, 1H), 7.59 -7.44 (m, 2H), 7.20 (s, 1H), 6.97 – 6.82 (m, 2H), 6.70 (s, 1H), 6.21 (d, J= 5.6 Hz, 1H), 4.95 (d, J= 5.6 Hz, 1H), 3.47 (s, 2H), 2.99 – 2.82 (m, 3H), 2.54 -2.48 (m, 4H), 2.43 – 2.20 (m, 9H), 0.94 (t, J= 7.2 Hz, 3H) ppm.MS: M/e 623 (M+1).

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

Reference£º
Patent; BEIGENE, LTD.; ZHOU, Changyou; ZHANG, Guoliang; WO2014/206343; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics