Heterocyclic Building Blocks-piperazine

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.

(6-Chloro-4,5-dimethyl-pyridazin-3-yl)-pyridin-2-yl-methanone (550 mg, 2.22 mmol), (R)-2-methyl-piperazine (320 mg, 3.20 mmol) are added into a microwave vial followed by NMP (6 mL) and triethylamine (0.92 mL, 6.66 mmol). The vial is sealed and irradiated in the microwave at 180¡ã C. for 1 h. The crude material is directly purified via flash chromatography on silica gel (20-70percent methanol in CH2Cl2) to afford the title compound (671 mg, 97percent). 1H NMR (400 MHz, DMSO-d6) delta=9.57 (br s, 1H), 8.66 (d, J=5.0 Hz, 1H), 8.10-8.17 (m, 2H), 7.69-7.73 (m, 1H), 3.65 (m, 1H), 3.62 (m, 1H), 3.45-3.50 (m, 1H), 3.12-3.33 (m, 4H), 2.29 (s, 3H), 2.15 (s, 3H), 1.32 (d, J=6.5 Hz, 3H).

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Novartis AG; US2010/41663; (2010); 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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of piperazine-1, 2-dicarboxylic acid 1-teit-butyl ester2-methyl ester (977 mg, 4.0 mmol) in DCM (20 mL) at 0 00 was added4-bromo-benzenesulfonyl chloride (1.02 mg, 4.0 mmol). Then TEA (404 mg, 4.0mmol) was added dropwise and the mixture was stirred at room temperature for 1hr. The mixture was concentrated and purified by silica gel chromatography(petroleum ether/EtOAc = 20/1 to 5/1) to afford 1.66 g (90%) of the titlecompound as a white solid. 1H NMR (400 MHz, ODd3) O [ppm] 7.69 (d, J = 8.8Hz, 2H), 7.61 (d, J= 8.8 Hz, 2H), 4.89-4.60 (m, 1H), 4.27-4.20 (m, 1H), 4.04-3.82(m, 1H), 3.77 (5, 3H), 3.76-3.61 (m, 1H), 3.35-3.11 (m, 1H), 2.51 (dd, J= 11.6, 4.0Hz, 1H), 2.33 (td, J= 11.6, 4.0 Hz, 1H), 1.44 (5, 9H).

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER INC.; ITEOS THERAPEUTICS; NINKOVIC, Sacha; CROSIGNANI, Stefano; SCALES, Stephanie Anne; MCALPINE, Indrawan James; COLLINS, Michael Raymond; MADERNA, Andreas; WYTHES, Martin; (295 pag.)WO2016/147144; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

STEP B: 2-ethyl-N-(3-fluoro-4-piperazin-1-yl-phenyl)-butyramide.To 4-(2-fluoro-4-methylamino-phenyl)-piperazine-1 -carboxylic acid tert- butyl ester prepared as in STEP A above and TEA (10.0 mmol) in CH2CI2 (50 mL) was added 2-ethyl-butyryl chloride (10.0 mmol). The resulting mixture was stirred at room temperature for 16 h. H2O (10 mL) was then added, the organic layer was separated. After concentration, the semi-solid was collected and re- dissolved into CF3COOH/CH2CI2 (10/50 mL). The resulting mixture was stirred at room temperature for 16 h, then concentrated to yield the title compound.

The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics