Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

In THF (50 mL) were dissolved 4-((3-chloro-4-methoxybenzyl)amino)-2-(5-azaspiro [2.4]heptan-5-yl)pyrimidine-5-carboxylic acid (1.0 g, 2.58 mmol), tert-butyl 4-(2-aminoethyl)piperazine-1-carboxylate (709 mg, 3.1 mmol) and HATU (1.18 g, 3.09 mmol). DIEA (1 mL, 5.16mmol) was added. The reaction was conducted at ambient temperature for 8 h. The solvent was removed, and DCM (50 mL) was added for resolution. The DCM phase was washed with water (50 mLx3). The organic phase was dried, concentrated and purified by silica gel column chromatography (DCM / methanol = 150/1) to give tert-butyl 4-(2-(4-((3-chloro-4-methoxybenzyl)amino)-2-(5-azaspiro[2.4]heptan-5-yl) pyrimidine-5-formamido)ethyl)piperazine-1-carboxylate as a white solid (910 mg, 59 percent yield)., 192130-34-0

As the paragraph descriping shows that 192130-34-0 is playing an increasingly important role.

Reference£º
Patent; Xuanzhu Pharma Co., Ltd.; WU, Frank; WANG, Aichen; EP2886540; (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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

General procedure: To a 10 ml microwave vial with stir bar was added amine (0.270 g, 1.5 equiv) and DABAL-Me3 (0.540 mg, 1.2 equiv). Reagents were suspended in THF (4 ml) and run in microwave reactor at 130 C for 20 min. The reaction mixture was cooled to room temperature and to it was added the appropriate Intermediate (0.500g. 1 equiv). The reaction mixture was irradiated in microwave reactor at 130 C for 20 min. After allowing to cool down to room temperature the reaction mixture was quenched by the addition of 2M HCl. The reaction mixture was extracted with ethyl acetate. The combined organic layer was washed with water (20 ml) and brine solution then dried over anhydrous sodium sulfate and evaporated under reduced pressure. The crude residue was purified by column chromatography using petroleum ether-ethyl acetate as eluents to get the pure amide.

109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK PATENT GMBH; SHERER, Brian; BRUGGER, Nadia; WO2015/130905; (2015); A1;,
Piperazine – Wikipedia
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55112-42-0,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55112-42-0,4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride,as a common compound, the synthetic route is as follows.

Benzyl N-(4-methylpiperazin-1-ylcarbonyl)glycinate may be prepared in the following manner: 4.2 cm3 of triethylamine and 3.02 g of benzyl glycinate hydrochloride are added, at 20 C., to 3 g of 4-methylpiperazin-1-ylcarbonyl chloride hydrochloride in solution in 150 cm3 of tetrahydrofuran. After stirring for 16 hours at 60 C., the reaction mixture is concentrated to dryness under reduced pressure (2.7 kPa) and the residue is taken up in 70 cm3 of dichloromethane. The organic phase is successively washed with twice 100 cm3 of a saturated aqueous sodium bicarbonate solution and 70 cm3 of water, and then dried over magnesium sulfate, filtered and concentrated to dryness under reduced pressure (2.7 kPa) to give 1.9 g of benzyl N-(4-methylpiperazin-1-ylcarbonyl)-glycinate in the form of a white solid. 1H NMR spectrum (400 MHz, (CD3)2SO d6, delta in ppm): 2.18 (s: 3H); 2.25 (t, J=5 Hz: 4H); 3.30 (t, J=5 Hz: 4H); 3.80 (d, J=6 Hz: 2H); 5.13 (s: 2H); 7.02 (t, J=6 Hz: 1H); from 7.30 to 7.45 (mt: 5H).

As the paragraph descriping shows that 55112-42-0 is playing an increasingly important role.

Reference£º
Patent; Aventis Pharma S.A.; US6569854; (2003); B1;,
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Piperazines – an overview | ScienceDirect Topics

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2,3-dichloro-1,4-naphthoquinone (0.37 g, 1.60 mmol) and 4-(4- methylpiperazin-1-yl)aniline (0.3 g, 1.46 mmol) was dissolved in EtOH (5 ml). The reaction was stirred and refluxed for 16 h. The residue was purified by flash column over silica gel (dichloromethane: methanol= 29: 1) to afford 77 (0.10 g, 17.30 %).1H NMR (300 MHz, CDCl3): delta 1.15 (t, J = 6.0 Hz, 3H), 2.48 (t, J= 6.0 Hz, 2H), 2.63 (t, J= 6.0 Hz, 4H), 3.26 (t, J= 6.0 Hz, 4H), 6.89 (d, J= 9.0 Hz, 2H), 7.03 (d, J= 8.7 Hz, 2H), 7.65-7.70 (m, 2H), 7.77-7.79 (m, 1H), 8.10- 8.13 (m, 1H), 8.18-8.20 (m, 1H).

115619-01-7, 115619-01-7 4-(4-Ethylpiperazin-1-yl)phenylamine 936738, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TAIPEI MEDICAL UNIVERSITY; YEN, Yun; LIOU, Jing-ping; PAN, Shiow-lin; (44 pag.)WO2017/20030; (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.197638-83-8,1-Boc-4-(4-Formylphenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 7 tert-Butyl 4-(4-(6-bromo-7-(4-((5-fluoropyridin-3-yl)methyl)piperazin-1-yl)-3H- imidazo[4,5-jb]pyridin-2-yl)phenyl)piperazine-1-carboxylateTo a mixture of 5-bromo-4-(4-((5-fluoropyridin-3-yl)methyl)piperazin-1-yl)-3- nitropyridin-2-amine (0.90 g, 0.22 mmol, 1 eq), EtOH (3.8 mL) and DMF (0.52 mL), tert-butyl-4-(4-formylphenyl)tetrahydro-1-(2H)pyrazine carboxylate (0.069 g, 0.24 mmol, 1.1 eq) was added followed by a freshly prepared aqueous solution of Na2S2O4 (1 M; 0.66 mL, 0.66 mmol). The reaction mixture was heated at 85 C for 24 h, then allowed to cool to room temperature and diluted with DCM and a few drops of aqueous NH3 until complete dissolution was observed. This solution was deposited on two preparative silica TLC plates and eluted with DCM/MeOH (v/v; 94:6). The title compound was obtained after trituration with diethyl ether as an off-white solid (0.025 g, 15%); 1H-NMR (500Mz, DMSO-Cf6): delta 1.42 (s, 9H, C(CH3J3), 2.59-2.67 (m, 4H, piperazine N(CH2)2), 3.23-3.29 (m, 4H, piperazine N(CH2)2), 3.43-3.52 (m, 4H, piperazine N(CH2)2), 3.60-3.70 (m, 6H), 7.07 (d, J = 9.0 Hz, 2H, ArH, C6H4), 7.70- 7.75 (m, 1 H, py 4-H), 8.13 (d, J = 9.0 Hz, 2H, ArH, C6H4), 8.18 (s, 1 H, imidazo[4,5- jb]pyridine 5-H), 8.45-8.48 (m, 1 H, py 2-H ), 8.50 (d, 1 H, J = 3.0 Hz, py 6-H)1 13.28 (brs, 1 H, imidazo[4,5-iotab]pyridine N-H); LC (Method B) – MS (ESI, m/z) 4.59 min – 651/653 [(M+H)+, Br isotopic pattern]. ESI-HRMS: Found: 651.2200, calculated for C3IH37FBrN8O2 (M+H)+: 651.2201.

197638-83-8, The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHROMA THERAPEUTICS LTD.; WO2009/1021; (2008); 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.1228780-72-0,1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine,as a common compound, the synthetic route is as follows.

Example 40G ethyl 2-(3-chlorophenoxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoate EXAMPLE 40A (1.2 g), EXAMPLE 40F (1.4 g), and HK2PO4 (0.9 g) were stirred in DMSO (2 mL) at 130 C. for 24 hours. The mixture was diluted with ethyl acetate, washed three times with water, washed with brine, dried, and concentrated. The concentrate was chromatographed on silica gel with 20% ethyl acetate/hexanes.

1228780-72-0, 1228780-72-0 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine 66713599, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ABBOTT LABORATORIES; US2010/184766; (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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

17.6 g of N- (4-aminophenyl) -N, 4-dimethyl-1-piperazineacetamide was addedMethyl N-acetyl-3- [methoxy (phenyl) methylene] -2-oxoindoline-6-carboxylate19g was added to DMF15 mL and 75 mL of methanol,Reflux reaction 1.5h or more.The reaction solution was added with 9.4 g of N-methylpiperazine,Reaction 1h,Cooling,Filtration to 5 C.Nidanibu products25.1g.250 ml of nidadibugar methanol was recrystallized,The purity of purified nidadipine was 99.58%

262368-30-9, 262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Ruiyang Pharmaceutical Co., Ltd.; Miao Dezu; Hu Qingwen; Cong Chao; Wang Hongguang; Yu Zhibo; (9 pag.)CN106748960; (2017); 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.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of (+/-)-tert-butyl 3-methylpiperazine-1-carboxylate (1.5 g), 1-fluoro-4-nitrobenzene (1.06 g) and potassium carbonate (2.07 g) in dimethyl sulfoxide (15 ml) was stirred at 120 C. for 15 hours. The reaction mixture was cooled to room temperature and poured into water (30 ml). The mixture was extracted with ethyl acetate three times. The combined organic layers were washed successively with water (twice) and brine, and dried over magnesium sulfate. The solvent was removed under reduced pressure. The residue was purified by silica gel column chromatography (hexane-ethyl acetate 2:1) to give the title compound as a white solid. [00322] 1H-NMR (300 MHz, CDCl3) delta 1.18 (d, J=5 Hz, 3H), 1.48 (s, 9H), 2.99-3.31 (m, 3H), 3.55 (td, J=2 Hz,9 Hz, 1H), 3.85-4.26 (m, 3H), 6.76 (d, J=8 Hz, 2H), 8.12 (d, J=8 Hz, 2H)., 120737-59-9

As the paragraph descriping shows that 120737-59-9 is playing an increasingly important role.

Reference£º
Patent; Fujisawa Pharmaceutical Co., Ltd.; US6825200; (2004); B1;,
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.1001180-21-7,(R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (1.0 g, 3.0 mmol, see Example 3) was dissolved in DCM (15 mL) in a plastic bottle, and then DAST was added neat over approximately 5 minutes. The reaction was quenched after 42 hours at room temperature by pouring into saturated aqueous sodium bicarbonate solution mixed with ice. The organic layer was diluted with EtOAc, washed 3 times with water, once with brine and then dried over sodium sulfate. After filtration, the residue was concentrated and purified via column chromatography (70:30 hexane/ethyl acetate, then 1:1 hexane/ethyl acetate) to give (R)-tert-butyl 4-(7,7-difluoro-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4- yl)piperazine-l-carboxylate (300 mg, 28%).

1001180-21-7, As the paragraph descriping shows that 1001180-21-7 is playing an increasingly important role.

Reference£º
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; WO2009/6567; (2009); A2;,
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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The above product 17C (460 mg, 1.66 mM) was dissolved in dichloromethane (10 mL), triethylamine (347 muL, 2.49 mM) and p-toluenesulfonyl chloride (317 mg, 1.66 mM) were added and reacted overnight. The reaction was monitored by TLC, and 5% citric acid aqueous solution was added, extracted with dichloromethane, washed with saturated brine, dried over anhydrous sodium sulfate, concentrated, and subjected to column chromatography (petroleum ether/ethyl acetate=2/1) to obtain 17D ( 600 mg, yield 84%)., 170911-92-9

The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chengdu Beisikairui Biological Technology Co., Ltd.; Li Dequn; (44 pag.)CN107540636; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics