Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure for 10-(amino)-6,ll-dihydro-5H-indeno[l,2- h]ll,6]naphthyridin-5-one (51): A mixture of 10-bromo compound (50) (94 mg, 0.3 mmol), amine (64 mg, 0.45 mmol), Pd2(dba)3 (5.5 mg, 0.006 mmol), S-X-Phos (7.2 mg, 0.015 mmol), sodium tert-butoxide (72 mg, 0.75 mmol) in DMF (4 ml) was degassed and then purged with nitrogen. The mixture was irradiated under microwave at 130 0C for 20 min. It was concentrated and purified on the silica gel column using 0 to 7% methanol and DCM. The residue obtained was further purified on the reverse phase column to provide final product (51).; 5.3 Examples; The following examples were prepared according to the methods, schemes and experimental described above.; Example 49: 10-(4-(2-methoxyethyl)piperazin-l-yl)-6,ll-dihydro-5H-indeno[l,2- h] [l,6]naphthyridin-5~one; MS: m/z 377.2 (M-H+)., 13484-40-7

The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; INOTEK PHARMACEUTICALS CORPORATION; JAGTAP, Prakash; PHAM-HUU, Duy-Phong; COHEN, Frederick; HU, Huiyong; WANG, Xiaojing; WO2010/77663; (2010); A2;,
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314741-39-4, (S)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

314741-39-4, To a solution of (S)-1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (500 mg, 2.05 mmol) in anhydrous dichloromethane (20 mL) at 0 C. was added triethylamine (311 mg 3.1 mmol) and acetyl chloride (0.16 mL, 2.25 mmol). The mixture was stirred for 30 minutes, and then the mixture was diluted with dichloromethane. The organic layer was washed with H2O, dried with MgSO4, filtered and concentrated under reduced pressure to provide the titled compound.

314741-39-4 (S)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 1501855, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Altenbach, Robert J.; Liu, Huaqing; Clapham, Bruce; Aguirre, Ana L.; Cowart, Marlon; Koenig, John R.; Sarris, Katerina; Scanio, Marc J.; Swinger, Kerren K.; Vasudevan, Anil; Villamil, Clara I.; Woller, Kevin R.; US2015/210720; (2015); A1;,
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934-98-5,934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 15-chloro-3-(3-fury)-N-[2-(4-methylpiperazin-1-yl)ethyl]-1H-indole-2-carboxamideA DMF solution (340 mL) containing the compound obtained in Production example 1-3 (11.6 g), 2-(4-methylpiperazin-1-yl)ethylamine (7.0 g) and HATU (18.5 g) was ice-cooled to 15¡ã C., and diisopropylethylamine (23.2 mL) was added thereto and the resulting solution was stirred overnight at room temperature.The reaction solution was poured into water (1.5 L), and the mixture was stirred at room temperature for 5 minutes.A precipitate was collected by filtration and washed with water and then dissolved in chloroform (600 mL).The chloroform layer was washed with a saturated aqueous sodium hydrogen carbonate solution and then dried over anhydrous magnesium sulfate.The solvent was distilled off under reduced pressure, and the resulting residue was purified by NH-silica gel column chromatography (hexane:ethyl acetate=2:1 to 1:3), whereby the title compound (8.8 g) was obtained as a pale yellow solid.1H-NMR (400 MHz, CDCl3, deltappm): 2.30 (3H, s), 2.32-2.50 (8H, m), 2.47 (2H, t, J=5.8 Hz), 3.51 (2H, dt, J=5.8 Hz, 5.8 Hz), 6.63 (1H, dd, J=1.9, 0.9 Hz), 7.03 (1H, br s), 7.25 (1H, m), 7.39 (1H, dd, J=8.8 Hz, 0.6 Hz), 7.49 (1H, m), 7.66 (1H, m), 7.70 (1H, m), 9.78 (1H, s).ESI-MS Found: m/z 387[M+H]+

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MSD K.K; US2012/28990; (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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

D. Amination Reaction In one experiment, (Benzotriazol-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate (41.73 g, 94.35 mmol) and triethylamine (88 mL, 630 mmol) were added to a mixture of (R)-2-(1-hydroxycyclohexyl)-2-(3-(trifluoromethoxy)phenyl)acetic acid (20.0 g, 62.9 mmol) and cis-2,6-dimethylpiperazine (7.17 g, 62.9 mmol) in methylene chloride (150 mL) at RT. After stirring for 18 h, the mixture was concentrated in vacuo. The residue was purified by flash chromatography on silica gel (50 to 100percent ethyl acetate in heptane) to afford 1-(3,5-Dimethyl-piperazin-1-yl)-2-(R)-(1-hydroxy-cyclohexyl)-2-(3-trifluoromethoxy-phenyl)-ethanone (24.3g, 93percent).

21655-48-1, As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference£º
Patent; Wyeth; US2007/135449; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

[00171]A mixture of 97 (0.30 g, 0.88 mmol), HBTU (0.50 g, 1.32 mmol), DIPEA (0.23 ml, 1.32 mmol) and DMF (2.5 ml) was stirred for a while, to which was then added 4-(4- ethylpiperazin-1-yl)aniline (0.27 g, 1.32 mmol) at room temperature and the mixture was stirred overnight. The residue was filtered by suction filtration to yield a red product. The residue was filtered without further purification to afford 37 (0.40 g, 85.92 %) as a red solid. 1H-NMR (300 MHz, DMSO-d6): ^1.01 (t, J= 7.2 Hz, 3H), 2.34 (q, J= 7.2 Hz, 2H), 3.07 (br, 4H), 5.01 (s, 2H), 6.89 (d, J= 9.0 Hz, 2H), 7.41 (d, J= 8.1 Hz, 2H), 7.56 (d, J= 9.0 Hz, 2H), 7.74 (t, J= 8.1 Hz, 1H), 7.77-7.88 (m, 3H), 7.95-7.98 (m, 2H), 8.09 (s, 1H), 9.98 (s, 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; (102 pag.)WO2017/14788; (2017); A1;,
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109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[Example 71] 1-[5-(5-Methylpyridin-2-yl)-1-(pyridin-3-yl)-1H-pyrazole-3-carbonyl]-4-methyl-3-oxopiperazine Triethylamine (0.330 mL) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (179 mg) were added at room temperature to a solution of 5-(5-methyl-2-pyridyl)-1-(3-pyridyl)-1H-pyrazole-3-carboxylic acid (0.218 g) obtained from Referential Example 9, 1-methyl-2-piperazinone hydrochloride (176 mg) obtained from Referential Example 15, and 1-hydroxybenzotriazole (143 mg) in N,N-dimethylformamide (15 mL), and the mixture was stirred at room temperature for 15.5 hours. The reaction solvent was evaporated under reduced pressure, and the residue was partitioned between ethyl acetate and saturated aqueous sodium hydrogencarbonate. The aqueous layer was further extracted with ethyl acetate four times. The organic layers were combined, and the combined organic layer was dried over sodium sulfate anhydrate. After a filtration step, the solvent was evaporated under reduced pressure, and the residue was purified by silica gel flash column chromatography (dichloromethane – methanol), to thereby give the title compound (231 mg, 78%) as a solid product. 1H-NMR(400MHz,CDCl3)delta:2.34(3H,s), 3.03(3H,s), 3.46-3.50(2H,m), 4.03-4.07(1H,m), 4.41-4.45(2H,m), 4.85(1H,brs), 7.16-7.20(1H,m), 7.34-7.40(2H,m), 7.52-7.56(1H,m), 7.68-7.83(1H,m), 8.30(1H,s), 8.47(1H,brs), 8.59(1H,brs). ESI-MS m/z:377(M+H)+. Elementary analysis: as C20H20N6O2 Calculated: C,63.82;H,5.36;N,22.33. Found: C,63.65;H,5.28;N,22.24.

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; DAIICHI PHARMACEUTICAL CO., LTD.; EP1762568; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

630125-91-6, A mixture of 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (7, 17.5 mg, 0.06 mmol), triethylamine (0.014 mL, 0.1 mmol), and p-nitrophenyl chloroformate (12.4 mg, 0.06 mmol) in 1,4-dioxane (5 mL) was heated at 60 C for 2 h. A solution of 6a (20 mg, 0.06 mmol) in 1,4-dioxane (5 mL) was slowly added thereto. The reaction mixture was heated at 90 C overnight. The reaction mixture was concentrated under reduced pressure and then partitioned between water (5 mL) and ethyl acetate (5 mL). The organic layer was separated and the aqueous layer was then extracted with ethyl acetate (3 ¡Á 3 mL). The combined organic extracts were washed with brine and dried over anhydrous Na2SO4. After evaporation of the organic solvent, the residue was purified by column chromatography (silica gel, hexane-ethyl acetate 3:1 v/v then switching to hexane-ethyl acetate 1:1 v/v) to yield compound 8g (6.0 mg, 15%).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference£º
Article; El-Gamal, Mohammed I.; Jung, Myung-Ho; Lee, Woong San; Sim, Taebo; Yoo, Kyung Ho; Oh, Chang-Hyun; European Journal of Medicinal Chemistry; vol. 46; 8; (2011); p. 3218 – 3226;,
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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

a) (S)-(+)-3-methyl-1-(2-nitrophenyl)piperazine. To a solution of 2-bromo-1-nitrobenzene (0.6 g, 3.0 mmol) in 1,4-dioxane (15 mL) was added (S)-(+)-2-methylpiperazine (0.5 g, 0.5 mmol) and powdered K2CO3 (15.0 mmol, 1.5 g) and the resulting suspension was heated at reflux for 10 h. After the suspension was cooled, it was filtered through a sintered glass funnel and the solvent was evaporated in vacuo. The resulting residue was purified by column chromatography on silica gel (1:1 hexane/EtOAc followed by 4:1 EtOAc/MeOH) to yield (S)-(+)-3-methyl-1-(2-nitrophenyl)-piperazine as an orange oil (0.53 g, 80%).

74879-18-8, The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Synaptic Pharmaceutical Corporation; US6245773; (2001); 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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

EXAMPLE 7 6-chloro-2-(4-cyclopropyl-1-piperazinyl)-pyrazine hydrochloride Crude N-cyclopropylpiperazine (2.8 g) and 2,6-dichloropyrazine (3.0 g) are combined in 5 ml 2,2,2-trifluoroethanol and the mixture refluxed 4 hours under N2. The mixture is concentrated under vacuum and the residue partitioned between aqueous sodium carbonate and methylene chloride. The combined methylene chloride extracts are extracted with dilute hydrochloric acid which is made basic with sodium hydroxide. The crude base is extracted with methylene chloride and chromatographed on silica gel. Elution with CHCl3 gives fractions containing 2.4 g pure title base which is treated with hydrogen chloride in ethanol-isopropanol to give 2.0 g of the title salt, mp greater than 340 C. with decomposition at 245 C., 20327-23-5

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

Reference£º
Patent; Merck & Co., Inc.; US4163849; (1979); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.

5308-25-8, 1-(bromomethyl)-4-nitro-2-(trifluoromethyl)benzene (34 g, 120 mmol) obtained in above was dissolved in dichloromethane (300 mL), followed by stirring. The reaction solution was added with 1-ethylpiperazine (15.97 mL, 126 mmol) and DIPEA (27.2 mL, 156 mmol), followed by further stirring for about 3 hours at room temperature. The reaction mixture was diluted with dichloromethane, and washed with a saturated aqueous solution of sodium bicarbonate and brine. The organic layer was dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain the title compound (21.7 g, 57%). -NMR Spectrum (300 MHz, DMSO-MS(ESI+, m/z): 318 [M+H]+

As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference£º
Patent; HANMI PHARM CO., LTD.; BAE, In Hwan; SON, Jung Beom; HAN, Sang Mi; KWAK, Eun Joo; KIM, Ho Seok; SONG, Ji Young; BYUN, Eun Young; JUN, Seung Ah; AHN, Young Gil; SUH, Kwee Hyun; WO2013/100632; (2013); A1;,
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Piperazines – an overview | ScienceDirect Topics