Month: April 2021

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 26A (3R)-3-methyl-1-pyridin-2-ylpiperazine (R)-(-)-2-Methylpiperazine (0.50 g, 0.005 mol, Aldrich) and 2-bromopyridine (5 mL, 0.05 mol) were combined and heated at 120¡ã C. for 14 hours. The reaction mixture was allowed to cool to 23¡ã C. and partitioned between a large volume of ethyl acetate and water. The layers were separated, and then additional water was added to the ethyl acetate solution. Drops of 1 N HCl solution were added to the water/ethyl acetate mixture with vigorous mixing. The layers were separated, and the combined aqueous phases were basified to pH ~11 with a solution of saturated sodium bicarbonate and solid sodium carbonate. Sodium chloride was added, and the saturated aqueous solution was extracted with chloroform containing a few drops of isopropyl alcohol (5*). The combined organic extracts were dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure to afford 0.79 g (89percent yield) of the title compound. 1H NMR (400 MHz, DMSO-d6) delta1.02 (d, J=6.0 Hz, 3H), 2.27 (dd, J=10, 12 Hz, 1), 2.67 (m, 3H), 2.92 (m, 1H), 4.07 (m, 2H), 6.58 (dd, J=6, 8 Hz, 1H), 6.77 (d, J=8 Hz, 1H), 7.49 (m, 1H), 8.08 (m, 1H); MS (ESI) m/e 178 (M+H)+., 75336-86-6

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

Reference£º
Patent; Cowart, Marlon D.; Bhatia, Pramila A.; Daanen, Jerome F.; Stewart, Andrew O.; Patel, Meena V.; Kolasa, Teodozyj; Brioni, Jorge D.; Rohde, Jeffrey; Engstrom, Kenneth M.; US2003/162790; (2003); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 3 (100 mg, 0.28 mmol), arylpiperazines or piperidines,K2CO3, (1.2 equiv), potassium carbonate (6.0 equiv) and CH3CN(25 mL) were placed in 50-mL round-bottomed flask equipped withmagnetic stirrer for 14 h at 85 C (monitored by TLC). After completionof reaction, the reaction mixture was filtered, and the filtrate wasconcentrated in vacuo. Then the residue was purified by chromatographyon silica-gel column (petroleum ether: ethyl acetate=5:1, v/v)to obtain the corresponding products (4-26), and all compounds wererecrystallized from dichloromethane and n-hexane.

30459-17-7, 30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Chen, Hong; Liang, Xue; Sun, Tao; Qiao, Xiaoguang; Zhan, Zhou; Li, Ziyong; He, Chaojun; Ya, Huiyuan; Yuan, Mu; Steroids; vol. 134; (2018); p. 101 – 109;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of NaOEt was prepared from NaH (60% dispersion in mineral oil) (0.723 g, 19 mmol) and 20 mL EtOH. To this solution was added diethyl carbonate (8.50 mL, 70 mmol) and the mixture was transferred to a solution of (R)-4-N-BOC-2-hydroxymethyl-piperazine (1.523 g, 7.0 mmol) in 80 mL of EtOH and heated at 78 C. After 6.5 h the reaction was cooled to RT and filtered. The filtrate was concentrated to dryness to give an off-white amorphous solid.

278788-66-2, The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Amgen Inc.; US2006/199817; (2006); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.132710-90-8,1-Boc-4-(3-hydroxypropyl)piperazine,as a common compound, the synthetic route is as follows.

2-Chloro-1-fluoro-4-nitrobenzene (320 mg) and sodium hydride (60% in oil, 83 mg) were added to a THF (3 mL) solution of tert-butyl 4-(3-hydroxypropyl)piperazine-1-carboxylate (310 mg) at room temperature, and the reaction mixture was stirred at 70C overnight. Water was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with water and saturated brine, was dried over sodium sulfate, and was then concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (eluent: hexane-ethyl acetate) to obtain the target compound. 1H-NMR (CDCl3) delta 1.46 (9H, s), 1.94-2.04 (2H, m), 2.36-2.44 (4H, m), 2.51 (2H, t, J = 7.1 Hz), 3.44 (4H, br-s), 4.11 (2H, t, J = 6.2 Hz), 6.87 (1H, dd, J = 9.2, 2.6 Hz), 7.03 (1H, d, J = 2.6 Hz), 8.00 (1H, d, J = 9.2 Hz). LCMS (B) RT 1.01, m/z [M+H] +400/402., 132710-90-8

The synthetic route of 132710-90-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Taiho Pharmaceutical Co., Ltd.; MINAMIGUCHI, Kazuhisa; OKAJIMA, Shigeo; ASAI, Takahiro; ASAI, Masanori; OGINO, Yoshio; (80 pag.)EP3381916; (2018); A1;,
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109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 68b; 1-Methyl-4- (4-nitro-benzyl)-piperazine; To a solution of 3 g (13.9 mmol) of 4-nitrobenzyl bromide (Flukla, Buchs, Switzerland) in 10 ml of DMF are added 3.08 ml (27.8 mmol) of N-methylpiperazine and 4.8 g (34.7 mrnol) of K2C03, and the mixture is stirred for 4.5 h at 80 C. After this time, 150 ml of EtOAc are added and the solution is washed with water, dried over MgS04, filtered and evaporated to dryness to provide the title compound. ES-MS: 236 (M+H) +.

109-01-3, 109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/54238; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of tert-butyl 4-carbamothioylpiperazine-1-carboxylate (synthesized according to Example 5, Step 1,2.0 g, 8.16 mmol) in dioxane (20 mL), TEA (1.7 mL,10.6 mmol) and 1-bromobutan-2-one (1.2 mL, 10 mmol) were added and stirred at 80C for 16 h. The completion of the reaction was monitored by TLC. The reaction mixture was quenched with water (10 mL) and extracted with EtOAc (2 x 25 mL). The organic layer was separated, dried over anhydrous Na2504, concentrated under vacuum. The resulting product was taken as such for next step. Yield: 86% (2.1 g, paleyellow solid). LCMS: (Method A) 298.0 (M+H), Rt. 2.94 mm, 93.1% (Max)., 196811-66-2

As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference£º
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; KULKARNI, Santosh, S.; GIRI, Awadut Gajendra; TORONTO, Dawn, V.; CROWE, David, Malcolm; (150 pag.)WO2017/144637; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

A. 1-methyl-4-[(4-nitrophenyl)methyl]piperazine To a solution of p-nitrobenzyl chloride (5.2 g, 10mM) and 3.2 g of triethylamine in 30 ml of ethylene glycol is added a solution of N-methylpiperazine (3 g, 30 mM) in 20 ml of ethylene glycol. After complete addition, the resulting solution is heated to 80 C. under nitrogen for 30 minutes. The reaction mixture is quenched into aqueous 10% sodium carbonate solution and extracted with methylene chloride. The methylene chloride solution is washed with water, saturated sodium chloride solution, dried over anhydrous sodium sulfate and concentrated to give 4.15 g (59%) of 1-methyl-4-[(4-nitrophenyl)methyl]piperazine.

109-01-3, As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Patent; The Upjohn Company; US4140775; (1979); A;,
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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

CuCO3.Cu(OH)2.H2O (15.8 g) was added to the H2O (275 mL) solution of piperazine-2-carboxylic acid, dihydrochloride (22.3 g), then the mixture was refluxed and stirred for 10 min. The insoluble material was filtered off and was washed with hot H2O (165 mL). The filtrate was cooled to room temperature, and NaHCO3 (9.2 g) and 1,4-dioxane (220 mL) was added to the dark blue solution. The mixture was cooled to 0 C. and NaHCO3 (18.5 g) and 50% solution of 4-nitrobenzyl chloroformate in 1,4-dioxane (61.7 g) was added to the mixture for 0.5 h. After stirring for additional 1.5 h at 0 C., the precipitate was filtered and washed with cold H2O (140 mL), EtOH (100 mL), acetone (200 mL) and Et2O (100 mL), then it was allowed to dry under reduced pressure to obtain the pale blue crystals. The crystals were added to the 1 mol/L HCl (330 mL) solution of EDTA.2Na (20.5 g) for 30 min, and stirred for 2 h at room temperature. The suspension was filtered and the filtered material was diluted with EtOH-H2O (7:3, 550 mL) and refluxed for 10 min. The reaction mixture was filtered to obtain the colorless crystals. The recrystallization from the filtrate was carried out 3 times to obtain additional crystals. The combined crystals were dried under reduced pressure to obtain the titled compound (26.25 g, 77%) as colorless crystals. 1H NMR (D2O) delta 2.54-2.61 (m, 1H), 2.89 (dt, 2H, J=12.7, 3.4 Hz), 2.97 (br, 1H), 3.13 (br, 1H), 3.62-4.04 (m, 2H), 5.16 (s, 2H), 7.49 (d, 2H, J=8.6 Hz), 8.14 (d, 2H, J=8.6 Hz).

3022-15-9, As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference£º
Patent; Wyeth; US2006/276445; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

373608-48-1, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

373608-48-1, Bis(trimethylsilyl)amide lithium (1 M in THF, 10,3 mL, 10.3 mmol) was added to a stirred suspension of 2-(2-fluoro-4-methoxyphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (0.679 g, 2.06 mmol) and 1-tert-butoxycarbonyl-4-(3-aminopropyl)piperazine (0.957 g, 3.93 mmol) in anhydrous THF (20 mL). After the addition was complete, the reaction was heated to reflux with stirring for 24 h. After that time the reaction was cooled to rt, diluted with saturated aqueous NH4CI (15 mL) and concentrated under reduced pressure. Saturated aqueous NaHC03 (SO mL) was added and the mixture was extracted with chloroform (4 x 30 mL). The combined organic layers were dried (MgSO4) and concentrated under reduced pressure. The product was purified by flash column chromatography (silica gel, 98:2 chloroform methanol) followed by recrystalization from chloroform/hexanes to give 5,7-dimethoxy-2-(4-methoxy-2-[3-(1-tert-butoxycarbonylpiperazin-4-yl)propylamino]phenyl)quinazolin-4(3H)-one (0.253 g, 22%) as a yellow solid:

The synthetic route of 373608-48-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Zenith Epigenetics Corp.; Quinn, J.F.; Khlebnikov, V.; (124 pag.)CN105593224; (2016); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.187669-60-9,1-(4-(Methylsulfonyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

Step 3: To a solution of 2-(6-bromopyridin-3-yl)-5-chloro-lH-berizimidazole (70mgs 0.227mmol) and l-[4-(meraylsulfonyl)phenyl]piperazine (54.5mgf 0.227mmol) in dry DMA (3mL) was added N,N-diisopropylethylamine (59mg, 0.454mmol). The mixture was heated to 110 C under argon for 16 hours. The mixture was filtered and was purified by reverse phase Prep HPLC using 30-60% C?CN/H2O/0.1%TFA as gradient to give 5-cMoro-2-(6-{4-(4- (methylsulfonyl)phenyl]piperazin-l-yl}pyridin-3-yl)-lH-benzimidazole as the TFA salt. LC-MS (M+H)= 468, 187669-60-9

187669-60-9 1-(4-(Methylsulfonyl)phenyl)piperazine 735904, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; SCHERING CORPORATION; SPERBECK, Donald, M.; DEVITA, Robert, J.; BALKOVEC, James, M.; GREENLEE, Mark, L.; WU, Zhicai; YU, Yang; VACHAL, Petr; ZHOU, Gang; WU, Heping; KUANG, Rongze; TING, Pauline; ASLANIAN, Robert; WO2012/64569; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics