Month: October 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.113028-17-4,Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 1 Ethyl 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4yl)methyl-1-piperazinyl]-4oxo-4H-[1,3-]thiazeto[3,2-a]quinoline-3-carboxylate. Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate (3.88 g) and 1.23 g of potassium bicarbonate were suspended in 20 ml of N,N-dimethylformamide, 2.38 g of 4-bromomethyl-5-methyl-1,3-dioxolen-2-one was dropped thereinto with ice cooling, and the mixture was stirred for 3 hours. After the reaction, the solvent was evaporated in vacuo therefrom at 50 C. and the residue was extracted with chloroform containing a few amount of methanol. The extract was washed with water, dried, the solvent was evaporated therefrom and the residue was purified by a column chromatography (chloroform-methanol/silica gel) to give 3.32 g of desired product. M.p. 241-243 C. (decompn.) Elem. Anal. for C23 H24 FN3 O6 S; Calcd. (%) C: 56.43 H: 4.94 N: 8.58; Found (%) C: 56.13 H: 4.99 N: 8.26. IR (KBr) nu (cm-1): 1820, 1720 (carbon-yl). NMR (CF3 CO2 D)(ppm) 1.51(3H, COOCH2 CH3, t), 2.31(3H, STR10 s), 2.35(3H, STR11 d), 3.40~4.30(8H, proton in piperazine ring, m), 4.55(2H, STR12 s), 4.65(2H, COOCH2 CH3, q), 6.51(1H, STR13 q), 7.05(1H, 8-proton, d), 8.11(1H, 5-proton, d).

113028-17-4, The synthetic route of 113028-17-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nipponshinyaku Co., Ltd.; US5086049; (1992); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57184-23-3, 1-(Cyclohexylmethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57184-23-3, 4-Cyclohexylmethyl-piperazine-1-carboxylic acid 4-(4-trifluoromethyl-phenoxy)-phenyl Ester The hydrochloride of the title compound was prepared from 4-(4-trifluoromethyl-phenoxy)-phenyl chloroformate and 1-cyclohexylmethyl-piperazine, yield 93%. White crystals, m.p. 256-258 C.; IR (KBr): nu 1715 (C=O) cm-1.

As the paragraph descriping shows that 57184-23-3 is playing an increasingly important role.

Reference£º
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); 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.

To a solution of 1 (0.31 g, 1.43 mmol) in THF (20 mL) was added Ti(OEt)4 (0.595 g, 2.58 mmol) and N-(4-trifluoromethylphenyl)-piperazine 2 (0.3 g, 1.3 mmol). The mixture was stirred at 40 C. for 24 h, quenched by adding ice-water, extracted with ethyl acetate (3¡Á20 mL), dried. Purification by column chromatography (PE/EA:1/1) gave product 3 (0.25 g, 41%).

30459-17-7, The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; COGNITION THERAPEUTICS, INC.; Catalano, Susan M.; Rishton, Gilbert; Izzo, Nicholas J.; (109 pag.)US2017/197977; (2017); A9;,
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.1383146-20-0,(R)-4-(2,4-Dimethoxybenzyl)-3-methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

General procedure: General Method I:General Method I is the procedure used for the synthesis of (R)-l-(2,4-dimethoxybenzyl)-5-ethoxy-6-methyl- l,2,3,6-tetrahydropyrazine (R)-D (cf. Scheme 30) as detailed below. Oven dried (115C) sodium carbonate (2.48 g, 23.40 mmol, 2.25 eq.) was placed in a round-bottom flask. The round-bottom flask was backfilled with Ar and then capped with a rubber septum. A solution of (R)-4-(2,4-dimethoxybenzyl)-3-methylpiperazin-2-one (R)-C (2.75 g, 10.40 mmol, 1 eq.) in anhydrous DCM (35 mL) was added, followed by freshly prepared triethyloxonium tetrafluoroborate (2.48 g, 13.05 mmol, 1.25 eq.) in one portion. Thereafter the reaction mixture was stirred further at RT for 1 hour, whereupon the reaction mixture was diluted with saturated aqueous NaHC03 (100 mL). The aqueous layer was extracted with DCM (3 x 200 mL). The organic layers were combined, dried over MgS04, filtered and concentrated under reduced pressure to afford 3.1 g of yellow oil. The crude compound was then purified on silica gel (EtOAc/MeOH: 99/1) to afford the desired product (R)-D as a pale yellow oil. Yield: 1.44 g, 48 %. LCMS: P = 95 , retention time = 1.8 min, (M+H20+H)+: 311 ; chiral HPLC retention time = 12.3 min, ee > 97 %. 1H-NMR (CDC13): delta 7.23 (d, J= 8.8, 1H), 6.48 (d, J= 8.8, 1H), 6.44 (s, 1H), 4.02 (m, 2H), 3.92 (s, 6H), 3.86 (d, JAB= 14.0, 1H), 3.46 (d, JAB= 14.0, 1H), 3.44 (m, 2H), 3.10 (m, 1H), 2.79 (m, 1H), 2.32 (m, 1H), 1.35 (d, J= 6.8, 3H), 1.24 (t, J= 6.0, 3H)., 1383146-20-0

The synthetic route of 1383146-20-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EUROSCREEN S.A.; HOVEYDA, Hamid; DUTHEUIL, Guillaume; FRASER, Graeme; ROY, Marie-Odile; EL BOUSMAQUI, Mohamed; BATT, Frederic; WO2013/50424; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-81-3, B. 1-methyl-4-[(4-aminophenyl)methyl]piperazine A suspension of 1-[(4-nitrophenyl)methyl]-4-methylpiperazine (3.5 g, 0.015 M) and 700 mg of 5% Pd/C in 200 ml of absolute ethanol is hydrogenated for 20 minutes. This is then filtered, washed with more ethanol and concentrated to a white oil. This is crystallized from acetate/Skellysolve B to give 900 mg (30%) of white crystalline 1-methyl-4-[(4-aminophenyl)methyl]piperazine.

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

Reference£º
Patent; The Upjohn Company; US4140775; (1979); A;,
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.350684-49-0,tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

KOtBu (2.81 g, 25.08 mmol) was dissolved into 20 ml DMSO in a round bottom flask, tert-butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate (7 g, 22.92 mmol) in 30 ml DMSO was added and the resulting mixture was stirred for 15 minutes at room temperature, then cooled in an iced bath for 5 minutes. 5-bromo-2- fluorobenzonitrile (4.6 g, 23.00 mmol) in 20 ml DMSO was added. The ice bath was removed and the mixture stirred for 5 hours while warming to room temperature. LCMS showed product and unreacted starting materials. Additional KOtBu (2g, 17.82 mmol) was added and the reaction stirred at room temperature overnight. The mixture was transferred into a separating funnel that was loaded with dichloromethane and dilute aq. NH4CI solution. The layers were separated, the organic layer washed one more time with water, then brine, dried over MgStheta4, filtered and concentrated in vacuum. The crude was dissolved in dichloromethane, and refluxed while adding ethyl acetate until the solution becomes cloudy, then allowed to stand and cool to room temperature. The product precipitated and was collected by filtration. 6.40 g tert-butyl 4-(4-(4-bromo-2-cyanophenylamino)- benzoyl)piperazine-1-carboxylate were isolated as a white solid. The mother liquor was concentrated in vacuum and purified by column chromatography on silica, gradient from 100% dichloromethane to 50% ethyl acetate in dichloromethane. Product containing fractions were combined and evaporate to give additional 0.90 g product as a pale yellow solid. MS (ESI) m/z 485/487 (1 Br isotope pattern) (M+H), 429/431 (1 Br isotope pattern) (M+H-C4H8). 1H NMR (CDCl3) delta ppm 7.64 (s, 1 H), 7.50 (d, 1H, J= 9.2), 7.42 (d, 2 H, J= 8.3), 7.19-7.15 (m, 3H), 6.39 (s, 1 H), 3.80- 3.40 (b, 8 H), 1.47 (s, 9H)., 350684-49-0

350684-49-0 tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate 2763355, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; PURANDARE, Ashok, Vinayak; BATT, Douglas, G.; LIU, Qingjie; JOHNSON, Walter, L.; MASTALERZ, Harold; ZHANG, Guifen; ZIMMERMANN, Kurt; WO2010/80474; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55112-42-0, 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55112-42-0, Example 1: Preparation of Zopiclone in Ethyl acetate[0064] To a slurry of l-chlorocarbonyl-4-methyl piperazine hydrochloride(CMP) (52.96g) in Ethyl acetate (500 ml), mechanically stirred, was added tri-ethyl amine (Et3N) (46.12g) over 10 min. During Et3N addition, temperature rose by 2C. After Et3N addition ended, DMAP (4.62g) and 6-(5-chloro-2-pyridinyl]-6,7-dihydro- 7-hydroxy-5H-pyrrolo[3,4-b]pyrazine-5-one (7-OH-Py) (5Og) were added to the slurry. Then the slurry was heated to 6O0C. The slurry was stirred at 600C for 7.5 h. The heating was stopped and the slurry was cooled to room temperature. When the temperature reached the room temperature water was added (500 ml) and the slurry was stirred for 1 h. The obtained solid was filtered, washed with acetone (25 ml) and dried in vacuum oven at 400C overnight to give zopiclone product crude (7 Ig yield 90%; purity 99.22%). Zopiclone crude can be purified by crystallization to get zopiclone of a purity greater than 99.8%.

The synthetic route of 55112-42-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/2629; (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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A vial was charged with palladium (II) acetate (0.012 g, 0.054 mmol) and 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (0.034 g, 0.054 mmol). Toluene (1.0 mL) was added and the system was flushed with argon. The vial was capped and the mixture stirred at room temperature for 15 min. A resealable tube was charged with 4-(4-chloro-3-phenyl-furo[2,3-b]pyridin-2-yl)-phenol (6) (0.174 g, 0.541 mmol), 4-N-(tert-butoxycarbonyl)-1-aminoethylpiperazine (0.248 g, 1.08 mmol), and potassium carbonate (1.495 g, 10.82 mmol). The Pd/BINAP solution was added along with 1.0 mL of toluene, and the system was flushed with argon. The tube was sealed and the mixture stirred at 130 C. for 15 h. The reaction mixture was partitioned between ethyl acetate and saturated aqueous sodium bicarbonate solution. The aqueous phase was separated and extracted with ethyl acetate. The combined organic phases were washed with saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate, filtered and concentrated to afford a brown solid. This material was purified via column chromatography on silica gel (eluting with 0-50% (90:10:1, dichloromethane/methanol/ammonium hydroxide)-dichloromethane) to afford 4-{2-[2-(4-hydroxy-phenyl)-3-phenyl-furo[2,3-b]pyridin-4-ylamino]-ethyl}-piperazine-1-carboxylic acid tert-butyl ester 7a as a tan solid. MS (MH+) 515.2; Calculated 514 for C30H34N4O4.

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

Reference£º
Patent; Nunes, Joseph J.; Martin, Matthew W.; White, Ryan; McGowan, David; Bemis, Jean E.; Kayser, Frank; Fu, Jiasheng; Liu, Jinqian; Jiao, Xian Yun; US2006/46977; (2006); 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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

b) 4-(5-Trifluoromethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl ester;To a solution of 17.5 mmol 2-benzenesulfonyl-3-trifluoromethyl-oxirane in 20 ml N,N-dimethylformamide was added 15.9 mmol 4-thiocarbamoyl-piperazine-l-carboxylic acid tert-butyl ester (prepared from tert-butyl 1-piperazinecarboxylate, 1,1′- thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054). The mixture was heated at 90 0C for 10 h. The reaction mixture was then concentrated in vacuo and the residue purified by chromatography (SiO2, ethyl acetate/heptane) to afford the title compound as an orange crystalline solid (yield 26%). MS (m/e): 338.1 (M+H+, 100%)., 196811-66-2

As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; WO2006/72436; (2006); 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.,3022-15-9

Method-B [0556] Alternatively the above prolinamide derivative can be prepared by the following method. [0557] DIEA (1.35 g, 10.46 mmol), HOBT (1.40 g, 10.37 mmol) sequentially added to piperazine acid (3.30 g, 10 mmol) and L-prolinamide (1.14 g, 10 mmol) in DCM (40 ml) at 0 C. A solution of DCC (2.40 g, 11.65 mmol) in DCM (30 ml) is added slowly at 0 C. over a period of 1 hr. Stirred another 1 hr. at 0 C. and then at 25 C. for 14 hrs. Filtered, DCM distilled off, diluted with ethyl acetate, washed sequentially with saturated aqueous solution of NaHCO3 and brine. Organic layer dried (Na2SO4), evaporated in vacuo purified by column chromatography (ethyl acetate). (Yield 2.6 g, 61.03%).

3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TORRENT PHARMACEUTICALS LTD.; US2004/106802; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics