Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

655225-01-7, Preparation 7.3N-Methyl-N-[2-(piperazin-1 -yl)ethyl]acetamide ditrifluoroacetate. 0.341 g of 60percent NaH in oil is added to a solution of 0.748 g of N- methylacetamide in 80 ml of THF and stirred for 10 minutes at RT. Then 2 g of fe/f-butyl 4-(2-bromoethyl)piperazinecarboxylate is added and stirred for 16 hours at RT. Water is added to the reaction mixture, it is decanted and the organic solvent is evaporated under vacuum. The residue is dissolved in DCM, filtered through a Chem Elut.(R). cartridge, eluting with DCM and the solvents are evaporated under vacuum. The residue is purified by preparative HPLC and a white solid is obtained. The solid is dissolved in 5 ml of DCM, 1 .2 ml of TFA is added and it is stirred for 16 hours at RT. The reaction mixture is diluted by adding 100 ml of toluene and the solvents are concentrated under vacuum.1 .5 g of the expected compound is obtained.

The synthetic route of 655225-01-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SANOFI; BADORC, Alain; BOLDRON, Christophe; DELESQUE, Nathalie; FOSSEY, Valerie; LASSALLE, Gilbert; YVON, Xavier; WO2012/146318; (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.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.

4-Cyclopropylmethyl-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-cyclopropylmethyl-piperazine, yield 43%. White crystals, m.p. 238-2390C; IR (KBr): nu 1725 (C=O) cm-1.

57184-25-5, As the paragraph descriping shows that 57184-25-5 is playing an increasingly important role.

Reference：
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.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A Pyrex yessel was charged with magnetic stirring bar. (2.0 g. 11.42 mmol) of 2-methoxy-4-(oxiran-2-yl) benzonitrile, (3.70 g, 17.12 mmol) of tert-butyl (3R)-3-(hydroxymethyl)piperazine- 1 -carboxylate, and 6 m of EtOH. Then it was introduced in the microwaye reactor and irradiated at 150 C for 3 h. The mixture was cooled to room temperature and the solyent was eyaporated and the resulting residue was purified by column chromatography (silica gel, 1- 20% dichloromethane/MeOH) which afforded the product as a mixture of twodiastereomers (1:1) LCIMS: (IE, miz) [(M + 1) – t-Bu]± = 336.41

278788-66-2, As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DE JESUS, Reynalda, Keh; DING, Fa-xiang; DONG, Shuzhi; FRIE, Jessica; GU, Xin; JIANG, Jinlong; SHAHRIPOUR, Aurash; PIO, Barbara; TANG, Haifeng; WALSH, Shawn; WO2014/126944; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

150407-69-5, (S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

11.2 g (34.9 mmol) TBTU and 5.5 mL (39.6 mmol) triethylamine were added to a mixture, cooled to 0 C., of 12.2 g (32.8 mmol) 1-benzyl-4-tert-butyl(S)-piperazine-1,2,4-tricarboxylate and 30 mL EtOH in 150 mL THF, stirred for another 30 min at this temperature and then stirred for 68 h at RT. 600 mL diethyl ether were added to the reaction mixture, it was combined with 200 mL saturated NaHCO3 solution, the aqueous phase was separated off, the organic phase was washed with saturated NaCl solution and dried over Na2SO4. After elimination of the desiccant and solvent the residue was purified by chromatography (silica gel, gradient PE/EtOAc 4:1 to 7:3). Yield: 11.35 g (88% of theory) ESI-MS: (M+H)+=393 Rf=0.38 (Polygram-silica gel, PE/EtOAc 3:1), 150407-69-5

As the paragraph descriping shows that 150407-69-5 is playing an increasingly important role.

Reference：
Patent; Mueller, Stephan Georg; Rudolf, Klaus; Lustenberger, Philipp; Schaenzle, Gerhard; Santagostino, Marco; Stenkamp, Dirk; Arndt, Kirsten; Doods, Henri; US2007/49581; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5625-67-2, Reference Example 3 4-(Tert-butoxycarbonyl)-2-piperazinone To a mixture of 2-piperazinone (3.00 g) and acetonitrile (50 ml) was added dropwise di-tert-butylbicarbonate (7.20 g), and the mixture was stirred at room temperature for 2 hours. The reaction solution was concentrated under reduced pressure, and precipitated crystals were washed with ether to give colorless crystals of the title compound (4.77 g). 1H-NMR (CDCl3) delta: 1.48 (9H, s), 3.33-3.43 (2H, m), 3.64 (2H, t, J=5.3 Hz), 4.09 (2H, s), 6.40-6.70 (1H, br). IR (KBr): 1696, 1667, 1400, 1341, 1130 cm-1.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference：
Patent; Takeda Chemical Industries, Ltd.; US6403595; (2002); 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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

Example 46 1-tert-Butyl 3-methyl 4-(1-benzhydrylazetidin-3-yl)piperazine-1,3-dicarboxylate A mixture of 1-benzhydrylazetidin-3-yl methanesulfonate (2.4 g, 7.56 mmol), tert-butyl methyl piperazine-1,3-dicarboxylate (1.85 g, 7.56 mmol), K2CO3 (1.6 g, 11.34 mmol) in CH3CN (40 mL) was stirred at reflux for 16 h. The mixture was partitioned between ethyl acetate and water. The organic layer was washed with water and brine, dried over Na2SO4, and concentrated in vacuo. The residue was purified by flash column chromatography on silica gel (10% petroleum ether/ethyl acetate) to afford the desired product (1.85 g, 51% yield)., 129799-08-2

The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Ren, Pingda; Liu, Yi; Li, Liansheng; Feng, Jun; Wu, Tao; US2014/288045; (2014); 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.,934-98-5

To a solution of 5-chloro-3-(4-methoxy-phenyl)-3 H-[ 1 ,2, 3]triazolo[4, 5-dJ- pyrimidine (200 mg, 0.76 mmol) in THF (4 ml) is added triethylamine (107 p1,0.76 mmol). The reaction mixture is stirred for 1 hour at room temperature. The reaction mixture is partitioned between dichioromethane and water. The organic phase is dried over sodium sulfate and evaporated. The residue is chromatographed on a silica gel column with dichloromethane/methanol toafford [3-(4-methoxy-phenyl)-3H-[1 ,2 ,3]triazolo[4,5-djpyrimid in-5-yl]-[2-(4- methyl-piperazin-1 -yl)-ethy]-amine as off-white powder; HPLC/MS 1.47 mm (A), [M+H] 369; 1H NMR (500 MHz, DMSO-d6) O [ppm] 9.22 (s, IH), 8.03 (d, J = 8.2 Hz, 2H), 7.92 (m, 1H), 7.17 (d, J = 9.0 Hz, 2H), 3.85 (s, 3H), 3.49?3.41 (m, 2H), 3.30 (m, 2H), 2.53 (m, 2H), 2.45 (m, 2H), 2.30 (m, 4H), 2.14 (s, 3H).

As the paragraph descriping shows that 934-98-5 is playing an increasingly important role.

Reference：
Patent; MERCK PATENT GMBH; DORSCH, Dieter; HOELZEMANN, Guenter; CALDERINI, Michel; WEGENER, Ansgar; POESCHKE, Oliver; WO2014/135244; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 28: (2,2-Dimethyl-piperazin-1yl)-[1-(3-fluoro-phenyl)-1H-[1,2,4]triazol-3yl]-methanone A mixture of 460 mg (2.22 mmol) 1-(3-fluoro-phenyl)-1H-[1,2,4]-triazole-3-carboxylic acid and 330 muL (2.49 mmol) 1-chloro-N,N,2-trimethylpropylamine in 10 mL THF was stirred at RT for 30 min, 500 mg (2.22 mmol) 3,3-dimethyl-piperazine-1-carboxylic acid tert-butyl ester and 620 muL (4.45 mmol) TEA were added and the mixture was stirred at RT for 1 h. The solvent was removed by distillation and the residue was purified by HPLC. yield: 205 mg (30%) ESI-MS: m/z=304 (M+H)+, 259808-67-8

As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference：
Patent; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; US2013/158042; (2013); 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

To a suspension of triphosgene (0.16 g, 0.53 mmol) and Na2C03 (0.67 g, 6.28 mmol) in DCM (10 ml) kept at 0 ocunder argon, 4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (0.45 g, 1.57 mmol) was added. Thereaction was monitored by HPLC (following the formation of 4-ethyl-piperazine-1-carboxylic acid [4-(4-ethylpiperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-amide by treating a sample of the reaction mixture with Nethylpiperazine).After 1 h, 6-lodo-2,3-dihydro-1 H-indole (0.39 g, 1.61 mmol) was added and the reaction was letunder stirring 1 h at r.t. The mixture was diluted with DCM (10 ml), washed with water (3 x 10 ml), dried overanhydrous Na2S04 and concentrated under vacuum. Purification by flash column chromatography (DCM/MeOH 95/5)5 afforded the product as yellow foam (0.68 g, 77%).1H NMR (600 MHz, DMSO-dG) o ppm 1.00 (br. s., 3 H) 2.12-2.48 (m, 10 H) 3.15 (t, J=8.61 Hz, 2 H) 3.55 (br. s., 2 H)4.13 (t, J=8.70 Hz, 2 H) 7.03 (d, J=7.88 Hz, 1 H) 7.26 (dd, J=7.69, 1.65 Hz, 1 H) 7.64 (d, J=8.61 Hz, 1 H) 7.83 (d,J=8.43 Hz, 1 H) 7.97 (d, J=2.01 Hz, 1 H) 8.24 (d, J=1.28 Hz, 1 H) 8.84 (s, 1 H).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; MENICHINCHERI, Maria; ANGIOLINI, Mauro; BERTRAND, Jay Aaron; CARUSO, Michele; POLUCCI, Paolo; QUARTIERI, Francesca; SALOM, Barbara; SALSA, Matteo; ZUCCOTTO, Fabio; WO2014/72220; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8,5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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 130C 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 94.2%). Compound P46: 5-(4-Ethylpiperazin-1 -yl)-2-nitroaniline; The compound was obtained by the method analogous to that described for Compound P42. Starting from 5-chloro-2-nitroaniline (1.50 g, 8.69 mmol), potassium carbonate (1.32 g, 9.56 mmol) and 1 -ethylpiperazine (1.98 g, 17.3 mmol) w 2 ml of DMF, 2.021 g of the title product in the form of a yellow solid were obtained (yield 92.9%). MS-ESI: (m/z) calculated for C12H19N4O2 [ + H]+: 251.15, found 251.1. 1H NMR (300 MHz, CDC ) delta 7.81 (d, J = 9,6 Hz, 1 H), 6.39 (dd, J = 9,6 Hz;2, 1 Hz 1 H), 6.22 (d, J = 2,1 Hz, 1 H), 3.31 (dd, J = 4,5Hz, 4,8Hz, 4H), 2,44 (dd, J = 4,5Hz, 4,8Hz, 4H) 2,35 (q, J = 7.2 Hz, 2H),1.02 (t, J = 7.2 Hz, 3H) ppm.

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

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