Sep 2021 News New learning discoveries about 1-Isopropylpiperazine

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

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-fluoronitrobenzene (5g, 35.4mmol) in THF (5OmL), 1- isopropylpiperazine (4.54g, 35.4mmol) and K2CO3 (7.35g, 53.2mmol) are added. The reaction mixture is stirred at room temperature overnight. The solvent is removed in vacuo and the residue is partitioned between EtOAc and water. The organic layer is washed with brine, dried over MgSO4, filtered and concentrated. The crude compound is purified by silica gel column chromatography using 99:1 and 98:2 DCM:NH3 (7M in MeOH) to give the title compound (8.2g, 94percent).

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

Reference:
Patent; GALAPAGOS N.V.; WO2007/138072; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

16 Sep 2021 News Brief introduction of 1-Isopropylpiperazine

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

1-lsopropylpiperazine (1.8 ml_, 12.7 mmol, 2 equiv) was added to a cold (5°C) solution of 2- chloro-5-nitropyridine (1 g, 6.3 mmol,) in DCM (5 ml_). The reaction mixture was allowed to warm to rt, stirred for 16 h, diluted with DCM and H2O. The aqueous layer was separated and extracted with DCM. The organic phase was washed with brine, dried (Na2SO4), filtered and concentrated to provide 1.58 g of he title compound as a yellow solid: ESI-MS: 251.2 [M+H]+; tR= 2.20 min.

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NOVARTIS AG; WO2009/141386; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

15 Sep 2021 News Analyzing the synthesis route of 1-Isopropylpiperazine

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

4318-42-7,4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2-(3-bromo-5-fluoro-phenyl)-3,3-dimethyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid methyl ester (0.41 g, 1.0 mmol), 1-isopropyl piperazine (0.64 g, 5.0 mmol), copper (I) iodidie (120 mg, 0.6 mmol), L-proline (69 mg, 0.6 mmol) and potassium hydroxide (33.6 mg, 0.6 mmol) in DMSO (2 mL) was stirred at 120° C. for 2 hours. Then treated with saturated ammonium chloride (20 mL), extracted with ether (100 mL). After removal of solvent, the residue was purified on flash silica gel chromatography (silica gel from QingDao, 200-300 mesh, glass column from Shanghai SD company) (40percent ethyl acetate/hexanes) to afford 2-[3-fluoro-5-(4-isopropyl-piperazin-1-yl)-phenyl]-3,3-dimethyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid ethyl ester (0.27 g, 60percent) as a white solid: LC/MS m/e calcd for C27H36FN3O2 (M+H)+: 454.6, observed: 454.3

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Chen, Li; Feng, Lichun; Huang, Mengwei; Liu, Yongfu; Wu, Guolong; Wu, Jim Zhen; Zhou, Mingwei; US2011/257151; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

15 Sep 2021 News Analyzing the synthesis route of 1-Isopropylpiperazine

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

4318-42-7,4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2-(3-bromo-5-fluoro-phenyl)-3,3-dimethyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid methyl ester (0.41 g, 1.0 mmol), 1-isopropyl piperazine (0.64 g, 5.0 mmol), copper (I) iodidie (120 mg, 0.6 mmol), L-proline (69 mg, 0.6 mmol) and potassium hydroxide (33.6 mg, 0.6 mmol) in DMSO (2 mL) was stirred at 120° C. for 2 hours. Then treated with saturated ammonium chloride (20 mL), extracted with ether (100 mL). After removal of solvent, the residue was purified on flash silica gel chromatography (silica gel from QingDao, 200-300 mesh, glass column from Shanghai SD company) (40percent ethyl acetate/hexanes) to afford 2-[3-fluoro-5-(4-isopropyl-piperazin-1-yl)-phenyl]-3,3-dimethyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid ethyl ester (0.27 g, 60percent) as a white solid: LC/MS m/e calcd for C27H36FN3O2 (M+H)+: 454.6, observed: 454.3

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Chen, Li; Feng, Lichun; Huang, Mengwei; Liu, Yongfu; Wu, Guolong; Wu, Jim Zhen; Zhou, Mingwei; US2011/257151; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 1-Isopropylpiperazine

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of compound 5a-b (2 mmol) in dry DCM (10 mL) was added K2CO3 (1.1 equiv, 2.2 mmol, 304 mg). The mixture was cooled with a bath of ice/water, and then the appropriate N-substituted piperazine (2 equiv, 4 mmol), dissolved in DCM (2 mL), was added slowly over 30 min. The mixture was then stirred at room temperature for two hours, diluted with DCM (10 mL), washed with water (10 mL) and then with brine (10 mL). The organic layer was dried (Na2SO4), filtered and concentrated in vacuo to give a brown residue that was purified by column chromatography to furnish the derivatives 6a-aq.

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Romagnoli, Romeo; Baraldi, Pier Giovanni; Carrion, Maria Dora; Cara, Carlota Lopez; Cruz-Lopez, Olga; Salvador, Maria Kimatrai; Preti, Delia; Tabrizi, Mojgan Aghazadeh; Shryock, John C.; Moorman, Allan R.; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Bioorganic and Medicinal Chemistry; vol. 20; 2; (2012); p. 996 – 1007;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13 Sep 2021 News New learning discoveries about 1-Isopropylpiperazine

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

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Compound 4 0.2 g (0.41 mmol) and 25 muL piperdine (0.82 mmol) was added to the 1.0 mL dried CH2Cl2.Anhydrous Na2CO3 20 mg was then added to the mixture, which was stirred for 12 h. The mixturewas washed with the distilled water, the organic phase was separated and dried over anhydrousNa2SO4, and then concentrated viarotary evaporation. The crude product was purified by silica gelchromatography with petroleum ether?acetone?strong ammonia water (v/v/v, 8/1/0.1) as the eluentto gain 0.18 g yellow solid compound 5a in 90percent yield.

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

Reference:
Article; Feng, Xiu E.; Wang, Qin Jin; Gao, Jie; Ban, Shu Rong; Li, Qing Shan; Molecules; vol. 22; 12; (2017);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13 Sep 2021 News Downstream synthetic route of 1-Isopropylpiperazine

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

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Example 75 N-{2- [3 -Fluoro-5- (4-isopropyl-piperazin- 1 -yl) -phenyl] -3 ,3 -dimethyl- 1 ,2,3 ,4- tetrahydro-quinoline-6-carbonyl}-methanesulfonamideA mixture of 2-(3-bromo-5-fiuoro-phenyl)-3,3-dimethyl-l,2,3,4-tetrahydro-quinoline-6- carboxylic acid methyl ester (0.41 g, 1.0 mmol), 1-isopropyl piperazine (0.64 g, 5.0 mmol), copper (I) iodidie (120 mg, 0.6 mmol), L-proline (69 mg, 0.6 mmol) and potassium hydroxide (33.6 mg, 0.6 mmol) in DMSO (2 mL) was stirred at 120 °C for 2 hours. Then treated with saturated ammonium chloride (20 mL), extracted with ether (100 mL). After removal of solvent, the residue was purified on flash silica gel chromatography (silica gel from QingDao, 200-300 mesh, glass column from Shanghai SD company)(40percent ethyl acetate/hexanes) to afford 2-[3-fiuoro-5-(4-isopropyl-piperazin-l-yl)-phenyl] -3,3- dimethyl-l,2,3,4-tetrahydro-quinoline-6-carboxylic acid ethyl ester (0.27 g, 60percent) as a white solid: LC/MS m/e calcd for C27H36FN3O2 (M+H)+: 454.6, observed: 454.3.

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

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; CHEN, Li; FENG, Lichun; HUANG, Mengwei; LIU, Yongfu; WU, Guolong; WU, Jim, Zhen; ZHOU, Mingwei; WO2011/128251; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

8 Sep 2021 News Simple exploration of 1-Isopropylpiperazine

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Compound P42: 5-(Morpholin-4-yl)-2-nitroaniline To the flask 2-amino-3-nitro-6-chloropyridine (1.50 g, 8.47 mmol), potassium carbonate (1.30 g, 9.32 mmol) and morpholine (10.5 ml, 119 mmol) were added. The reaction was carried out under argon flow at 130°C overnight. The progress of the reaction was monitored by TLC (system: heptane/ethyl acetate, 1 /1 ). The mixture was cooled to room temperature and poured into the ice-water. A precipitated yellow solid was filtered and dried. 1.789 g of the title product were obtained (yield 94.2percent). Compound P58: 2-Nitro-3-[4-(propan-2-yl)piperazin-1 -yl]aniline; The compound was obtained by the method analogous to that described for Compound P42. Starting from 3-chloro-2-nitroaniline (0.459 g, 2.61 mmol), potassium carbonate (0.368 g, 2.66 mmol) and 1 -isopropylpiperazine (1.00 g, 0.741 mmol), 0.602 g of the title product in the form of a red solid were obtained (yield 91.9percent). MS-ESI: (m/z) calculated for Ci3H2iN402 [M + H]+: 265.16, found 265.1 1H NMR (500 MHz, DMSO-d6) delta 7.10 (dd, J = 8.1 Hz, 1 H), 6.52 (dd, J = 8.3, 1.0 Hz, 1 H), 6.35 (dd, J = 8.0, 1.0 Hz, 1 H), 5.83 (s, 2H), 2.85 (dd, J = 17.4, 12.8 Hz, 4H), 2.68 – 2.60 (m, 1 H), 2.47 (dd, 4H), 0.97 (d, J = 6.5 Hz, 6H).

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; CELON PHARMA S.A.; ZDZALIK, Daria; LIPNER, Joanna; WIECZOREK, Maciej; DZWONEK, Karolina; YAMANI, Abdellah; DUBIEL, Krzysztof; LAMPARSKA-PRZYBYSZ, Monika; GRYGIELEWICZ, Paulina; STANCZAK, Aleksandra; WO2014/141015; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

7 Sep 2021 News Some tips on 1-Isopropylpiperazine

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 2-(5-iodomethyl-2-oxo-oxazolidin-3-yl)-N-(6-methoxy-2-methyl-quinolin-4-yl)-acetamide (12, 0.2 g, 0.439 mmol), potassium carbonate (0.151 g, 1.09 mmol), different substituted amines (1.1 mmol) in 10 mL of acetonitrile was heated to 80 °C for 4 h. The reaction completion was monitored by TLC and when the reaction was completed, the reaction mass was filtered through a celite bed, filtrate was concentrated under reduced pressure. The crude residue was purified using biotage parallel column purifier using ethyl acetate in petroleum ether (4:1) to 4-6percent methanol in dichloromethane as eluant. The spectral data for the final compounds, 13a-n is given below.

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference:
Article; Thomas; Adhikari, Airody Vasudeva; Chowdhury, Imran H.; Sandeep; Mahmood; Bhattacharya; Sumesh; European Journal of Medicinal Chemistry; vol. 46; 10; (2011); p. 4834 – 4845;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

2 Sep 2021 News Some tips on 1-Isopropylpiperazine

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of tert-butyl 4-hydroxypiperidine-1-carboxylate (4.4 g, 21.9 mmol) in 0CM (100 mL) was carefully added OMAP (5.3g, 43.Bmmol) and triphosgene (3.2g. 10.95 mmol) portionwise. After stirring at ft for 2h, 1-isopropylpiperazine (3.3g. 26 mmol) was added and the reaction mixture was stirred at ft for 5 h. The reaction was quenched with saturatedNH4CI (100 mL) solution and the mixture was extracted with 0CM (3×1 00 mL). The combined organic layers were washed with saturated NH4CI (2×100 mL) and brine (SOmL) sequentially, dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure to afford thetitle compound as a white solid (7.7g. 99%). [LCMS: Rt1.67min, mz 356.3 (M + H)1., 4318-42-7

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; NOVARTIS AG; AUBERSON, Yves; BOCK, Mark Gary; BRAGA, Dario; CURZI, Marco; DODD, Stephanie Kay; GIAFFREDA, Stefano Luca; JIANG, Haiyang; KARPINSKI, Piotr; TROXLER, Thomas J.; WANG, Tielin; WANG, Xiaoyang; ZHANG, Xuechun; WO2014/13469; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics