Month: April 2021

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.

548762-66-9, To a stirred solution of tert-butyl (2S,5R)-2,5-dimethylpiperazine-1-carboxylate (0.35 g, 1.63 mmol) in acetonitrile (8 mL) were added DIPEA (0.9 mL, 4.9 mmol) and methyl 2-bromo-2-(5-(trifluoromethyl)pyridin-2-yl)acetate (0.54 g, 1.79 mmol) at room temperature. The reaction mixture was heated at 85 C for 16 h. The reaction mixture was cooled to room temperature, concentrated under reduced pressure to obtain the crude product, which was purified by silica gel chromatography (24 g; using 6 % -10 % ethyl acetate/ petroleum ether) to obtain tert-butyl (2S,5R)-4-(2-methoxy-2-oxo-1-(5- (trifluoromethyl)pyridin-2-yl)ethyl)-2,5-dimethylpiperazine-1-carboxylate (0.52 g, 74 % yield). LCMS: m/z = 432.2 (M+H); retention time 2.19 min [LCMS method: Column: Waters Acquity UPLC BEH C18 (2.1 x 50 mm), 1.7 mm; Mobile phase A: 0.1% TFA in water; Mobile phase B: 0.1 % TFA in acetonitrile; Gradient = 20-90 % B over 1.1 minute, then a 0.6 minute hold at 90 % B; Temperature: 50 C; Flow rate: 0.7 mL/min; Detection: UV at 220 nm].

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

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); 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.692058-21-2,1-Boc-4-(2,2,2-trifluoroethyl)piperazine,as a common compound, the synthetic route is as follows.

692058-21-2, tert-Butyl-l-piperazinecarboxylate (1.00 g, 5.37 mmol) and pyridine (0.868 mL, 10.7 mmol) were combined in methylene chloride (27 mL) and cooled to 0 C. Trifluoroacetic anhydride (0.910 mL, 6.44 mmol) was then added and the reaction mixture was allowed to warm to ambient temperature and stirred 1 h. The reaction mixture was then diluted with ethyl acetate (150 mL) and washed with aqueous potassium hydrogen sulfate (2 x 50 mL), saturated aqueous sodium bicarbonate (50 mL) and brine (50 mL), then dried over sodium sulfate and evaporated to yield tert-butyl 4-(2,2,2-trifluoroacetyl)piperazine-l-carboxylate (1.50 g, 99%) as an oil which solidified over time. tert-Butyl 4-(2,2,2-trifluoroacetyl)piperazine-1-carboxylate (0.908 g, 3.22 mmol) was added to a solution of borane-tetrahydrofuran complex (8 mmol) in tetrahydrofuran (24 mL) and the reaction mixture was heated at reflux for 2 h. After cooling, 2 N hydrochloric acid (4 mL) was carefully added and the reaction mixture was stirred until gas evolution ceased and then diluted with ethyl acetate (200 mL). Aqueous sodium hydroxide (0.2 M, 75 mL) was then added and the phases were separated. The organic layer was dried over sodium sulfate and evaporated. The residue was purified by column chromatography (eluting with 20% ethyl acetate in hexanes) to give tert-butyl 4-(2,2,2-trifluoroethyl)piperazine-1-carboxylate (0.627 g, 73%) as a white solid. A solution of hydrochloric acid (4.0 M, 10 mL) in dioxane was added to a solution of tert-butyl 4-(2,2,2-trifluoroethyl)piperazine-l-carboxylate (0.736 g, 2.74 mmol) in dioxane (5 mL). The reaction mixture was stirred until analysis by thin layer chromatography indicated completion of reaction (approx. 3 h). The volatiles were evaporated and the residue was dried under vacuum to yield 1- (2,2,2-trifluoroethyl)piperazine (0.631 g, 95%) as a white solid.

The synthetic route of 692058-21-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F.HOFFMANN-LA ROCHE AG; WO2005/110996; (2005); 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

The compound (R) -4-Boc-2- methylpiperazine (528mg, 2.64mmol), glacial acetic acid (190mg, 3.16mmol), 1-ethyl-3- (3- Dimethylaminopropyl) carbodiimide hydrochloride (758mg, 3.95mmol) and N- hydroxy-7-azabenzotriazole(897mg, 6.59mmol) was dissolved In dichloromethane (20 mL), and under conditions of 0 C tothis solution was added dropwise N, N- diisopropylethylamine (1.8mL, 10.54mmol), stirred at roomtemperature Stirred 12h, was added water (10mL ¡Á 2) washing the organic phase was dried over anhydrous Na 2SO 4, the solvent was removed concentrate was separated by column chromatography (leaching Lotion: DCM /MeOH (v / v) = 40/1), to give 580mg colorless oil: Compound N- acetyl-4-tert-butoxycarbonyl -2- (R) – methylPiperazine, yield: 90%., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
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.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

2-[(4-Bromo-2-fluoro-phenyl)methyl]-6-phenyl-thiazinane 1,1-dioxide (208 mg, 0.52 mmol), Pd(OAc)2 (5.8 mg, 0.026 mmol), 2-dicyclohexylphosphine-2?,6?-di-iso-propoxy-1,1?-biphenyl (24.8 mg, 0.052 mmol) and cesium carbonate (254 mg, 0.78 mmol) were weighed out in a vial and the vial was purged with nitrogen. 1,4-Dioxane (2.5 mL) and 1-piperazin-1-ylethanone (100 mg, 0.78 mmol) were then added and the reaction was stirred at 80 C. for 2 hours. The reaction was then filtered through diatomaceous earth, concentrated and purified by reverse-phase HPLC to give 1-(4-(4-((1,1-dioxido-6-phenyl-1,2-thiazinan-2-yl)methyl)-3-fluorophenyl)piperazin-1-yl)ethanone (210 mg, 89% yield)., 13889-98-0

The synthetic route of 13889-98-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Genentech, Inc.; Fauber, Benjamin; Gobbi, Alberto; Rene, Olivier; van Niel, Monique Bodil; Gancia, Emanuela; Gaines, Simon; Ladduwahetty, Tammy; Vesey, David; Ward, Stuart; Winship, Paul; (101 pag.)US2016/168141; (2016); 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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,75336-86-6

Solid Na2CO3 (200 mg, 1.9 mmol, 1.9 eq) is added to a solution of l-benzyl-4- chlorophthalazine (250 mg, 0.98 mmol, 1 eq) and (i?)-2-methyl-piperazine (400 mg, 4.0 mmol, 4.0 eq) in dioxane (5 mL) in a microwave vial. The vial is sealed and irradiated in the microwave at 150 0C (high absorption setting) for 30 minutes. The reaction mixture is filtered and concentrated, then diluted with EtOAc (50 mL) and water (15 mL). The organic fraction washed with water and then brine, then is dried over sodium sulfate. The solvent is evaporated under reduced pressure to afford the title compound as a white solid (180 mg, 58 percent yield).IH NMR (400 MHz, CHLOROFORM-^) delta ppm 8.08 (d, J=7.07 Hz, 1 H) 8.00 (d, J=7.71 Hz, 1 H) 7.69 – 7.79 (m, 2 H) 7.34 – 7.39 (m, 2 H) 7.25 – 7.32 (m, 2 H) 7.20 (d, J=7.20 Hz, 1 H) 4.61 – 4.65 (m, 2 H) 3.76 – 3.82 (m, 2 H) 3.13 – 3.30 (m, 4 H) 2.85 (dd, ./=12.63, 10.23 Hz, 1 H) 1.17 (d, J=6.32 Hz, 3 H) MS (m/z, MH+): meas. 319.1

As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; WO2008/110611; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of compound 9 (200mg, 0.8mmol), sodium iodine (289mg, 1.93mmol) and substituted amines (1.61mmol) in methanol (30mL) was stirred at 40C for 5h. After the reaction was completed (monitored by TLC), the solution was concentrated under vacuum. Then the crude residue was purified by column chromatography (dichloromethane/methanol), affording pure product 10., 208167-83-3

208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Liang, Yu-Kun; Yue, Zhi-Zhou; Li, Jia-Xin; Tan, Cun; Miao, Ze-Hong; Tan, Wen-Fu; Yang, Chun-Hao; European Journal of Medicinal Chemistry; vol. 84; (2014); p. 505 – 515;,
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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

mixture of tert-butyl 2-methylpiperazine- I -carboxylate (0.077 mL, 0.383 mmol), rac-(6S,7R,8R)-5-acetyl-6-cyclopropyl-7-methyl-8-(phenylamino)-5,6,7,8-tetrahyd ro- I ,5-naphthyridin-2-yltrifluoromethanesulfonate (for a preparation see Intermediate 102, 90 mg, 0.192 mmol) and cesium carbonate (187 mg, 0.575 mmol) in 1,4-dioxane (7 mL) had nitrogen bubbled through it for 10 mm. BINAP (23.87 mg, 0.038 mmol) and Pd2(dba)3 (17.55 mg, 0.019 mmol) were added and the reaction mixture was stirred at 90 C under nitrogen for 3 h. The reaction mixture was allowed to cool to rtthen filtered through celite, rinsed with ethyl acetate and concentrated under a stream of nitrogen. The sample was dissolved in 1:1 MeOH:DMSO (2×1 mL) and purified by MDAP (HpH). The appropriate fractions were combined and concentrated in vacuo. The sample was dissolved in DMSO:MeOH (1:1, 1 mL) and purified by MDAP (Formic). The appropriate fractions were combined and concentrated in vacuo to give the product (11 mg, 0.021 mmol, 11.04%) as a yellow gum. Thiswas a racemic mixture of diastereoisomers. LCMS (2 mm Formic): Rt = 1 .40 mi [MH] = 520.

120737-78-2, As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; AMANS, Dominique; ATKINSON, Stephen John; HARRISON, Lee Andrew; HIRST, David Jonathan; LAW, Robert Peter; LINDON, Matthew; PRESTON, Alexander; SEAL, Jonathan Thomas; WELLAWAY, Christopher Roland; WO2014/140076; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of substituted piperazine (10 mmol), 4-uoroben-zaldehyde (10 mmol) and K2CO3 (2 mmol) were reuxed at130 C in DMF for 15-24 h. Thereafter, the reaction mixture waspoured into ice cold water and the precipitate that appeared wasltered and dried to accomplish formyl derivatives (14-25) in ayield of 80-90%, 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Article; Mishra, Chandra Bhushan; Manral, Apra; Kumari, Shikha; Saini, Vikas; Tiwari, Manisha; Bioorganic and Medicinal Chemistry; vol. 24; 16; (2016); p. 3829 – 3841;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a mixture of 1-benzoylpiperazine (1.0 eq) and potassium carbonate (2.0 eq) in dimethylformamide was added dropwise a solution of the corresponding substituted 9-bromo-9H-fluorene (1.0 eq) in dimethylformamide (The synthesis of 9-bromo-9H-fluorene derivatives is reported in supporting information). After stirring for 24 h at room temperature, solvent was removed and the crude residue was dissolved in diethyl ether, washed with brine, dried over magnesium sulfate,filtered and concentrated under vacuum. The residue was purified by flash chromatography as indicated in each case to afford the title compound. Reagents: 1-Benzoylpiperazine (0.15 mmol, 29 mg), potassium carbonate (0.30 mmol, 42 mg) and 9-bromo-2-hexyl-9H-fluorene (0.15 mmol, 50 mg). The crude product was purified by flash chromatography (isocratic, petroleum ether/ethyl acetate 80/20) to afford a yellow oil (66 mg, 99%). TLC Rf: 0.34 (petroleum ether/ethyl acetate 80/20). IR (cm-1): 697, 708, 739, 766, 1001, 1137, 1256, 1277, 1426, 1455, 1632, 1674, 1715, 2854, 2925. HPLC: method 2, rt = 2.67 min purity 98%. 1H NMR (300 MHz, CDCl3) delta (ppm): 0.93 (t, J = 7.2 Hz, 3H); 1.24-1.48 (m, 6H); 1.63-1.76 (m, 2H); 2.44 (s, 2H); 2.72 (t, J = 7.8 Hz, 2H); 2.91 (s, 2H); 3.38 (s, 2H); 3.84 (s, 2H); 4.88 (s, 1H); 7.23 (dd, J = 1.5 Hz, 7.5 Hz, 1H); 7.29 (td, J = 1.2 Hz, 7.5 Hz, 1H); 7.34-7.42 (m, 6H); 7.46 (s, 1H); 7.61 (d, J = 7.5 Hz, 1H); 7.63 (d, J = 7.5 Hz, 1H); 7.67 (d, J = 7.5 Hz, 1H). 13C NMR (75 MHz, CDCl3) delta (ppm): 14.1 (CH3); 22.7 (CH2); 29.0 (CH2); 31.8 (2 * CH2); 36.2 (CH2); 43.0 (CH2); 48.5 (CH2); 48.8 (CH2); 49.7 (CH2); 69.9 (CH); 119.5 (CH); 119.6 (CH); 125.9 (CH); 126.0 (CH); 126.7 (CH); 127.1 (2 * CH); 128.3 (CH); 128.4 (2 * CH); 128.5 (CH); 129.6 (CH); 135.9 (C); 138.7 (C); 141.2 (C); 142.4 (C); 143.3 (C); 143.6 (C); 170.3 (C). MS (DCI/CH4) m/z: 438.27 [M]. HRMS (DCI/CH4): for C30H34N2O [M]: calcd: 438.2671; found: 438.2660., 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; Chollet, Aurelien; Mori, Giorgia; Menendez, Christophe; Rodriguez, Frederic; Fabing, Isabelle; Pasca, Maria Rosalia; Madacki, Jan; Kordulakova, Jana; Constant, Patricia; Quemard, Annaik; Bernardes-Genisson, Vania; Lherbet, Christian; Baltas, Michel; European Journal of Medicinal Chemistry; vol. 101; (2015); p. 218 – 235;,
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.

Sodium hydride (60percent, 0.87 g, 21.80 mmol) was added to diglyme (10 mL). A solution of 2-(4-methyl-piperazin-1-yl)-ethanol (3.14 g, 21.80 mmol) in diglyme (10 mL) was added slowly. The reaction mixture was heated at 40 00 for 1 hour, 4-chloro-pyridin- 2-ylamine (1.40 g, 10.9 mmol) was added and the reaction mixture was heated at 8000 for 1 hour, then at 15700 for 16 hours. The reaction mixture was cooled, diluted with water (20 mL), and THF (20 mL) was added, then NaCI. The organic phase was separated, and the aqueous phase was extracted with THF. The combined organic phase was dried, and the solvent was evaporated. Diethyl ether was added to the residue. The resulting solid was filtered, washed with ether, and dried to afford a white solid (1.86 g, 72percent), (M+H)=237.

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; SAXTY, Gordon; MURRAY, Christopher William; BERDINI, Valerio; PAGE, Lee William; ROOMANS, Susan; TAMANINI, Emiliano; BUCK, Ildiko Maria; DAY, James Edward Harvey; CARR, Maria Grazia; LEE, Lydia Yuen Wah; WO2015/4481; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics