Month: August 2020

57184-25-5, 1-(Cyclopropylmethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

9.8 g N,N-dibenzyl-4-amino-cyclohexanone was dissolved in 100 mL dichloromethane and stirred with 5.6 g N-cyclopropylmethylpiperazine and 8.5 g NaBH(OAc)3 for 12 h at RT. Then the mixture was combined with water and potassium carbonate, the org. phase was separated off, dried and the solvent was eliminated in vacuo. The residue was separated off using a silica gel column (approx. 50 mL silica gel, approx. 3 L ethyl acetate 95/methanol 5+0.25% conc. ammonia). The suitable fractions were evaporated down in vacuo. The desired compound was crystallised from ethanol+conc. HCl. Yield: 8.5 g of the compound Z9a.

57184-25-5 1-(Cyclopropylmethyl)piperazine 965875, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; Boehringer Ingelheim International GmbH; US2006/46989; (2006); A1;,
Piperazine – Wikipedia
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934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 6-nitrobenzo[d]oxazole-2-thiol (KR-200) (11.63 mmol, 2.28 g) in dichloromethane (465 mL) and oxalyl chloride (14.54 mmol, 1.25 mL) was placed under argon atmosphere and cooled to 0 ?C. Dimethylformamide (12 mL) was added drop wise over a period of 40 minutes. CAUTION: The addition of dimethylformamide should be conducted slowly to avoid rapid evolution of gas. The reaction was stirred for 30 minutes at 0 ?C, then ice bath was removed and the reaction was allowed to warm to room temperature. After two hours, the reaction was again cooled to 0 ?C and triethylamine (34.90 mmol, 4.87 mL) was added drop wise over a period of 25 minutes. Then 2-(4-methylpiperazin-1-yl)ethan-1-amine (KR-251) (12.80 mmol, 1.83 g) was added, and the ice bath was removed. The reaction was stirred for sixteen hours at room temperature then concentrated in vacuo yielding a red solid. Silica gel column chromatography of the solid (10:1 dichloromethane/methanol) provided pure KR-202251 as a yellow powder in a 53percent yield.

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various.

Reference£º
Article; Rynearson, Kevin D.; Charrette, Brian; Gabriel, Christopher; Moreno, Jesus; Boerneke, Mark A.; Dibrov, Sergey M.; Hermann, Thomas; Bioorganic and Medicinal Chemistry Letters; vol. 24; 15; (2014); p. 3521 – 3525;,
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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

A suspension of 1-fluoro-4-nitrobenzene (1.096 g, 7.77mmol), 1-cyclopropylpiperazine (1.00 g, 7.92 mmol) andpotassium carbonate (1.61 g, 11.65 mmol) in anhydrous DMF(10 mL) was heated to 50 C under a nitrogen atmosphereovernight. The reaction mixture was allowed to cool toroom temperature and poured into ice-water (50 mL) . Theprecipitated solid was isolated by filtration, washed with water and sucked dry to give the title compound as a yellow solid (1.11 g, 58%) . ?H NMR (500 MHz, CDC13) : 3 8.12 (d, 2H), 7.01 (d, 2H), 3.47 (t, 4H), 2.80 (t, 4H),1.70-1.80 (m, 1H), 0.45-0.60 (m, 4H) . LCMS (Method C):= 0.51 mi m/z = 248 [M+H].

20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ALMAC DISCOVERY LIMITED; HARRISON, Timothy; TREVITT, Graham; HEWITT, Peter Robin; O’DOWD, Colin Roderick; BURKAMP, Frank; WILKINSON, Andrew John; SHEPHERD, Steven D.; MIEL, Hugues; WO2015/92431; (2015); 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-(4-fluorophenylthio)propyl methanesulfonate (4b) (1.0 g, 3.79 mmol), 4-(4-chloro-phenyl)-piperidin-4-ol (0.8 g, 3.79 mmol), KI (120 mg), K2CO3 (1.2 g, 8.7 mmol) in DME (10 mL) was heated to reflux under N2 for 12 h. The cooled mixture was then diluted with EtOAc (400 mL) and washed with H2O (200 mL). The organic layers were pooled, dried with Na2SO4, and filtered. The filtrate was concentrated in vacuo, then followed by purification through column chromatography on silica gel, to afford 4-(4-chlorophenyl)-1-(3-((4-fluorophenyl)thio)propyl)piperidin-4-ol (6); yield 74%,

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

Reference£º
Article; Peprah, Kwakye; Zhu, Xue Y.; Eyunni, Suresh V.K.; Setola, Vincent; Roth, Bryan L.; Ablordeppey, Seth Y.; Bioorganic and Medicinal Chemistry; vol. 20; 3; (2012); p. 1291 – 1297;,
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74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 9 General Procedure: Palladium Catalyzed Coupling to Heteroaryl Chloride 2-Chloro-nicotinonitrile (1.0 mmol), (S)-2-methyl piperazine (1.5 mmol), sodium tert-butoxide (1.5 mmol) and tris(dibenzylideneacetone)-dipalladium(0) (0.04 mmol) were added to a screw cap vial. 2,8,9-Triisobutyl-2,5,8,9-tetraaza-1-phospha-bicyclo[3.3.3]undecane (0.08 mmol) was dissolved in toluene (5 mL) and this solution was added to the other reagents. The reaction mixture was stirred at 100 C. overnight. The solution was diluted with dichloromethane and washed with water. The organic phase was dried, filtered and concentrated, then purified by flash chromatography in 10% (2M ammonia in methanol) in dichloromethane to yield the desired product. In this manner the following compounds were synthesized: Example Structure Name Yield 9.1 2-[(3S)-3-methylpiperazin-1-yl]nicotinonitrile 64%1H 1.03(d, J=6.3 Hz, 3H); 1.73(s, broad, 1H); 2.59(dd, J=12.9, 10.2 Hz, 1H); 2.94(m, NMR 4H); 4.16(m, 2H); 6.64(dd, J=7.8, 4.8 Hz, 1H); 7.66(dd, J=7.8, 2.1 Hz, 1H); 8.23(dd, J=4.8, 2.1 Hz, 1H).

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference£º
Patent; AstraZeneca AB; NPS PHARMACEUTICALS; US2007/49578; (2007); 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.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

The dichloropyrimidine (2.30 gm, 6.98 X 10″3 moles) was dissolved in methylene chloride and N-methyl-N’-(2-aminoethyl)piperazine (1.0 gm, 6.98 X 10″3 moles) was added. After stirring at room temperature for 1 hour, TLC (silica, 10percent methanol in methylene chloride) showed some remaining starting material (Rf = 0.91) along with a single product (Rf = 0.32). Diisopropylethylamine (0.902 gm, 1.22 mL, 6.98 X 10″3 moles) was added and this solution was heated at 45¡ãC. for 90 minutes. After cooling, the methylene chloride was removed under reduced pressure and the remaining material was purified by chromatography on silica using 15percent methanol in methylene chloride as eluent. The fractions containing the product were pooled and evaporated to provide 2.1 gm (69percent>) of the product as an orange solid.

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; JANUS BIOTHERAPEUTICS, INC.; LIPFORD, Grayson, B.; ZEPP, Charles, M.; WO2012/167053; (2012); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

A suspension of 1-methyl-4-(4-nitrobenzyl)piperazine (1.0 g, 4.25 mmol), Pd/C (200 mg) in EtOH (20 mL) was stirred at room temperature under H2 (1 atm) for 6 h, then filtered, removed the solvent to give 4-((4-methylpiperazin-1- yl)methyl)aniline as light brown solid (785 mg), yield 90%. LC/MS (ESI) m/z = 206 (M + H)+.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Patent; THE BROAD INSTITUTE, INC.; DANA-FARBER CANCER INSTITUTE, INC.; THE GENERAL HOSPITAL CORPORATION D/B/A MASSACHUSETTS GENERAL HOSPITAL; GRAY, Nathanael, S.; LIANG, Yanke; CHOI, Hwan, Geun; SUNDBERG, Thomas; SHAMJI, Alykhan; XAVIER, Ramnik; FISHER, David E.; (251 pag.)WO2018/9544; (2018); A1;,
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4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step B. To a solution of 5-bromo-2-(3,4-dichloro-phenoxy)-pyridine (0.303 g, 0.949 mmol) in THF (4 mL) was added 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU; 0.30 mL, 2.0 mmol), cyclopropyl piperazine (0.30 mL, 2.4 mmol), trans-di-m-acetatobis[2-(di-o-tolylphosphino)benzyl]di-palladium (II) (Hermann’s catalyst; 36.7 mg, 0.039 mmol), t-BuPHBF4+ (17.4 mg, 0.060 mmol), and Mo(CO)6 (301 mg, 1.14 mmol). The reaction mixture was heated in the microwave for 6 min at 125¡ã C., cooled to rt, then concentrated. Purification by FCC gave the desired product (284 mg, 76percent). MS (ESI): mass calcd. for C19H21C12N3O2, 393.10; m/z found, 394.7 [M+H]+. 1H NMR (CDCl3): 8.24 (dd, J=2.5, 0.8 Hz, 1H), 7.83 (dd, J=8.3, 2.5 Hz, 1H), 7.47 (d, J=8.8 Hz, 1H), 7.30 (d, J=2.8 Hz, 1H), 7.03 (dd, J=8.8, 2.5 Hz, 1H), 7.00 (dd, J=8.3, 0.8 Hz, 1H), 3.90-3.40 (br m, 4H), 2.74 (h, J=6.8 Hz, 1H), 2.64-2.43 (br m, 4H), 1.04 (d, J=7.1 Hz, 6H).

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference£º
Patent; Keith, John M.; Letavic, Michael A.; Ly, Kiev S.; Mani, Neelakandha S.; Mills, John E.; Pandit, Chennagiri R.; Villani, Frank J.; Zhong, Hua; US2007/281923; (2007); 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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

To the round bottom flask was added 3-iodo-4-methyl-benzoic acid (2.62 g, lOmmol), 10 ml of thionyl chloride and refluxed at 78 C for 4 hours. The rotary evaporator removed the volatile material to give 3-iodo- 4-methyl-benzoyl chloride. A solution of 4- (4-methylpiperazin-1-ylmethyl) -3-trifluoromethylaniline (2.27 g, 8.3 mmol), 3-iodo-4-methyl-benzoyl chloride (LOmmol), 15 ml of tetrahydrofuran, 10 ml of triethylamine and stirred at room temperature for 4 hours. Washed with saturated NaHC03 solution, extracted with ethyl acetate and water, washed with saturated NaCl solution, dried over anhydrous Na2S04, and the solvent was removed by distillation under reduced pressure. The residue was purified by silica gel column to give the title compound.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; NANJING SANHOME PHARMACEUTICAL CO., LTD.; WANG, YONG; ZHAO, LIWEN; CHEN, HONGYAN; ZHANG, DI; XU, XIN; ZHANG, CANG; ZHANG, HONGXING; (9 pag.)CN103664951; (2016); B;,
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.

1-[4-(5-Bromo-2-methyl-benzoyl)-piperazin-1-yl]-ethanone To a mixture of 5-bromo-2-methylbenzoic acid (2.0 g, 9.30 mmol) in DCM (25 mL) was added DIPEA (3.25 mL, 18.60 mmol) and HBTU (4.23 g, 11.16 mmol) at rt. The reaction mixture was stirred at rt for 20 min. To the mixture was then added 1-(piperazin-1-yl)ethanone (1.311 g, 10.23 mmol) and the reaction mixture was stirred at rt for 1 hour. The reaction was quenched with a saturated aqueous solution of NaHCO3 and extracted with DCM. The organic layer was washed twice with brine, dried by passing through a phase separating cartridge and evaporated. Purification by Flash chromatography using Biotage Isolera system (amine functionalized silica KP-NH, eluting with Cyclohexane/EtOAc 0 to 100%) gave the title compound (2.475 g, 82% yield) as a white foam. MS: 325.4 [M+1], Rt(2)=0.94 min.

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

Reference£º
Patent; NOVARTIS AG; COOKE, Nigel Graham; FERNANDES GOMES DOS SANTOS, Paulo Antonio; FURET, Pascal; HEBACH, Christina; HOGENAUER, Klemens; HOLLINGWORTH, Gregory; KALIS, Christoph; LEWIS, Ian; SMITH, Alexander Baxter; SOLDERMANN, Nicolas; STAUFFER, Frederic; STRANG, Ross; STOWASSER, Frank; TUFFILLI, Nicola; VON MATT, Anette; WOLF, Romain; ZECRI, Frederic; US2015/342951; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics