Month: October 2020

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

General Procedure 3-1 : Synthesis of (4-((4-methylpiperazin-l-yl)methyl)aniline)[00187] The synthesis of the title compound was conducted as described in U.S. Pat. Appl. Publ.No. 2006058341 (March 16, 2006). Specifically, to a solution of 4-nitrobenzyl chloride in THF at the room temperature was added 1 -methyl piperazine. The solution was stirred for 3 hours after which time the crude reaction was diluted with ethyl acetate and washed repeatedly with water. The dried organics were concentrated to give directly the 4-nitrobenzylamine adduct.This was subsequently treated with Rainey Nickel in THF at 75PSI for 12 hours to give the title compound., 70261-81-3

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

Reference£º
Patent; BIOGEN IDEC MA INC.; WO2008/94575; (2008); 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.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Boc-2-S-ethyl piperazine 22 (prepared as per Kiley et al Org. Prep. Proc- Int. 1990, 22, 761 ; 4.2 g, 18.6 mmol), tris(dibenzylideneacetone)dipalladium (340 mg, 0.37 mmol), racemic-2,2′-bis(diphenylphosphino)-1 ,1′-binaphthyl (BINAP) (495 mtf, 0.74 mmol), cesium carbonate (12 g, 37.2 mmol) and toluene (80 ml). After the mixture was heated at 100 0C for 16 h, fresh tris(dibenzylideneacetone)- dipalladium (340 mg, 0.37 mmol) and BINAP (495 mg, 0.74 mmol) were added and the heating was continued for 3 days. The solvent was removed in vacuo, and the residue was suspended in a 100 ml portion of ethyl acetate. This mixture was extracted with water and brine. The separated organic layer was dried over sodium sulfate and concentrated in vacuo. Purification of the residue via silica gel flash chromatography (5percent methanol/ 95percent DCM) yielded 5.3 g of a partially purified material 23 which was used directly in the next step. M.S. M+H = 350

325145-35-5, As the paragraph descriping shows that 325145-35-5 is playing an increasingly important role.

Reference£º
Patent; SCHERING CORPORATION; PHARMACOPEIA, INC.; WO2007/109238; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8,59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-(4-oxo-3,4-dihydro-phthalazin- 1 -yl-oxyl)benzoic acid (54 mg, 0.3 mmol) was dissolved in N,N-dimethylformamide, and then 1-(3-dimethylaminopropyl)-3-ethylcar- bodiimide hydrochloride (EDCI) (220 mg, 1.2 mmol), triethylamine (150 pL, 1.2 mmol) and 1 -hydroxy-7-azaben- zotriazole (HOAt) (165 mg, 1.2 mmol) were added successively. The mixture was stirred at room temperature for half an hour, and then N-(cyclopropanecarbonyl) piperazine was added and reacted at room temperature overnight, and then the reaction was quenched with water, extracted with ethyl acetate, and washed with water for three times. The organic phases were combined and washed with saturated saline, dried with anhydrous sodium sulfate, and concentrated for colunm chromatography isolation (dichloromethane:methanol=20: 1) to give Compound 7. A white solid was obtained. ?H NMR (600 MHz, DMSO-d5): oe 11.98 (s, 1H), 8.27 (d, 1H, J=7.38 Hz), 8.10 (d, 1H, J=7.74 Hz), 7.99-8.01 (m, 1H), 7.94-7.96 (m, 1H), 7.52 (t, 1H, J=7.86 Hz), 7.39-7.38 (m, 2H), 7.28 (d, 1H, J=7.62 Hz), 3.33-3.81 (m, 8H), 1.96 (brs, 1H), 0.69-0.74 (m, 4H); ESI-MSm/z: calculated for4l8.16. found 417.89 [M-H].

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Patent; CHENGDU DI’AO PHARMACEUTICAL GROUP CO., LTD.; Ji, Jianxin; Guo, Na; Xue, Ting; Kang, Bingqiang; Ye, Xinfa; Chen, Xin; Zhang, Tao; US2015/51211; (2015); 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.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 5 Ethyl 7-(4-acetonyl-1-piperazinyl)-6-fluoro-1-methyl-4-oxo-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate Ethyl 6-fluoro-1-methyl-7-(1-piperazinyl)-4-oxo-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate (3.8 g) was suspended in 50 ml of N,N-dimethylformamide, 1.66 g of potassium carbonate was added thereto, 1.65 g of bromoacetone was dropped in with ice cooling and stirring, and the mixture was stirred at room temperature for 20 hours. The reaction solution was poured over into ice water and the crystals separated out were collected by filtration, washed with water, dried and recrystallized from ethanol to give 3.7 g of desired compound in colorless powdery crystals, m.p. 196-200 C. (decompn.). Elementary analysis calculated for C21 H24 FN3 O4 S: Calcd (%): C 58.18, H 5.58, N 9.69. Found (%): C 57.93, H 5.39, N 9.46., 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; Nippon Shinyaku Co., Ltd.; US4843070; (1989); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

169447-70-5, To a solution of 2,6-difluorobenzonitrile (0.8g, 5.7 mmol) in DMF (10 mL) was added (S)-tert-butyl 2-methylpiperazine-l-carboxylate (1.14 g, 5.7 mmol) and K2CO3 (2.35g, 17. Immol). The solution was stirred for 17 hrs at 100C, then concentrated to give the crude. The crude was purified by chromatography (silica, EtOAc/PE = 1/10) to afford (S)-/er/-butyl-4-(2- cyano-3-fluorophenyl)-2-methylpiperazine-l-carboxylate (0.6 g, 1.88 mmol, 33%) as a white solid. MS (EI+, m/z): 320 [M+H]+.

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; NAVITOR PHARMACEUTICALS, INC.; O’NEILL, David John; SAIAH, Eddine; KANG, Seong Woo Anthony; BREARLEY, Andrew; BENTLEY, Jonathan; (184 pag.)WO2018/89493; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

215309-01-6, 3-(4-Methylpiperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of 3-(4-methylpiperazin-1-yl)benzoic acid (0.58 g, 2 mmol) in dichloromethane (50 mL) and DMF (2 drops), oxalyl chloride (0.9 mL, 10 mmol) was added dropwise at RT. After addition the reaction mixture was heated at 60 C. for 2 h. After concentration and stripping with toluene the crude acyl chloride was dissolved in dry THF (7 mL)/triethylamine (3 mmol) and t-butylglycinate (0.286 mL, 2.1 mmol) was added at RT and the reaction mixture was stirred at RT overnight. After concentration obtained 0.66 g (2 mmol, quant.) of tert-butyl N-[3-(4-methylpiperazin-1-yl)benzoyl]glycinate. The above obtained t-butyl ester (0.1 g, 0.3 mmol) was stirred at RT in dichloromethane (4 mL) and trifluoroacetic acid (3 mL) overnight. The solvents were removed under reduced pressure and the crude material stripped three times with toluene. Obtained the corresponding acid (0.080 g. 96% yield). The acid was then reacted as described in Example 1 to afford the title compound. H-NMR (DMSOd6), delta ppm: 2.87 (s, 3 H) 3.13-4.03 (m, 8 H) 7.24-7.95 (m, 6 H) 8.36 (dd, J=4.63, 1.59 Hz, 1 H) 8.52 (d, J=2.44 Hz, 1 H) 9.11 (d, J=7.32 Hz, 1 H) 10.48 (s, 1 H) 11.83-11.96 (m, 1 H) 12.58 (s,1 H), 215309-01-6

As the paragraph descriping shows that 215309-01-6 is playing an increasingly important role.

Reference£º
Patent; Pharmacia Italia S.p.A.; US2007/112020; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of methyl (Z)-1-acetyl-3-(ethoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate (6) (500 mg,1.368 mmol) in DMF (3.5 mL) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (14) (395 mg,1.505 mmol, 1.1 equiv.) at RT. After heating the reaction mixture at 80 C for 1 h, it was allowed to cool to RT. Piperidine (297 lL,3.010 mmol, 2.2 equiv.) was then added and stirred for 2 h. Volatiles were removed in vacuo and water was added to the obtained residue and stirred for 15 min. The precipitate was then filtered under suction and cake was washed with water, then with minimum amount of cold methanol, and then ether. The obtained product was purified by column chromatography (neutral Al2O3,0-10% methanol in CH2Cl2) to afford 532 mg (72%) of target molecule 15. Major conformer 1H NMR (400 MHz, DMSO-d6): d 12.22 (s,1H), 10.98 (s, 1H), 7.66-7.47 (m, 5H), 7.42 (s, 1H), 7.24-7.09 (m,3H), 6.89 (d, J = 8.0 Hz, 2H), 5.83 (d, J = 8.0 Hz, 1H), 3.77 (s, 3H),3.06 (s, 3H), 2.69 (s, 2H), 2.34-2.06 (brs, 8H), 2.10 (s, 3H). HRMSm/z found 540.2606, calcd for C31H34N5O4 [M+H]+ 540.2605.

262368-30-9, As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference£º
Article; Edupuganti, Ramakrishna; Taliaferro, Juliana M.; Wang, Qiantao; Xie, Xuemei; Cho, Eun Jeong; Vidhu, Fnu; Ren, Pengyu; Anslyn, Eric V.; Bartholomeusz, Chandra; Dalby, Kevin N.; Bioorganic and Medicinal Chemistry; vol. 25; 9; (2017); p. 2609 – 2616;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

142-64-3, Piperazine Dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

100 g (1.2 mol) of anhydrous piperazine and 240 g (1.5 mol) of piperazine dihydrochloride were heated to 120 C.110 g (1.2 mol) of 2-chloroethanol was added dropwise, and heating and stirring were continued after the addition.The temperature was raised to 136-140 C for 1 hour, and TLC showed that the reaction was stopped and the heating was stopped.When the temperature drops to 80 degrees Celsius, add 500 ml of 95% ethanol and cool in the refrigerator overnight.Piperazine dihydrochloride was recovered by filtration the next day, the filter cake was washed well with a small amount of ethanol, and the filtrate was combined.Adding 200 g of 30% sodium hydroxide solution to alkalization, filtering out the insoluble inorganic salts;After the solvent was removed by concentration, the residue was evaporated to ethylamine.The solid content has beenMore than 98%.After recrystallization from a 90% aqueous solution of ethanol, 180 g of white crystals can be obtained in a yield of 85%.The content can reach more than 99.5%., 142-64-3

The synthetic route of 142-64-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nanjing Haiyan Bio-pharmaceutical Technology Co., Ltd.; Bu Gonggaofamingren; (4 pag.)CN109384742; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of commercially available (R)-3-methyl-piperazine-1-carboxylic acid tert-butyl ester (8.78 g, 44 mmol) in CH2Cl2 (80 mL) at 0 C. were added Et3N (12.15 mL, 88 mmol) and methanesulfonyl chloride (5.09 mL, 66 mmol). Stirring was continued at RT overnight, the reaction was poured onto water and extracted with CH2Cl2. The combined organic phases were dried on Na2SO4 and concentrated under vacuo. The crude product was dissolved in CH2Cl2 (50 mL) and TFA (15 mL) was added. After 2 hours at RT, the volatiles were removed under vacuo, the crude was dissolved in CH2Cl2 and washed with aq. NaHCO3 (until pH=8). The organic phase was dried on Na2SO4 and concentrated under vacuo to yield 2.63 g (34%) of (R)-1-methanesulfonyl-2-methyl-piperazine as a light yellow oil., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference£º
Patent; Jablonski, Philippe; Kawasaki, Kenichi; Knust, Henner; Limberg, Anja; Nettekoven, Matthias; Ratni, Hasane; Riemer, Claus; Wu, Xihan; US2009/54644; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

848482-93-9, (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N-(Methylcarbamoyl)-L-valine (2.0 g, 11.4 mmol) was dissolved in DMF (15 mL) at room temperature. HATU (4.34 g, 11.4 mmol) and di/sopropyl ethylamine (1.47 g, 1 1.4 mmol) were added and stirring was continued. After 10 minutes, solid piperazine-1,3-dicarboxylic acid l-tert-butyl ester (2.62 g, 1 1.4 mmol) was added. To the resultant suspension was added DMF (10 mL) and diwopropyl ethylamine (1.47 g, 11.4 mmol). Stirring at room temperature was continued. After 45 min, HATU (4.34 g, 11.4 mmol) and diwopropyl ethylamine (1.47 g, 11.4 mmol) were added to the resultant yellow solution followed by amino-(4’bromo) acetophenone hydrochloride salt (2.85 g, 11.4 mmol). After 30 minutes all volatiles were removed in vacuo. The crude material was taken into EtOAc and the organic layer was washed with aqueous HCl (1 M), aqueous LiCl (5%), aqueous bicarbonate solution, brine and was dried over sodium sulfate. Filtration and evaporation of solvents in vacuo yielded crude material, which was purified by flash chromatography on silica gel (eluent: EtOAc w MeOH 10%/ hexanes) to yield the product 3-[2-(4-Bromo-phenyl)-2-oxo- ethylcarbamoyl]-4-(2-methoxycarbonylamino-3-methyl-butyryl)-piperazine- 1 -carboxylic acid tert-butyl ester (3.62 g): LCMS-ESI+: calc’d for C25H35BrN4O7: 583.4 (M+); Found: 583.2 / 585.2 (M+H+).

848482-93-9, As the paragraph descriping shows that 848482-93-9 is playing an increasingly important role.

Reference£º
Patent; GILEAD SCIENCES, INC.; GUO, Hongyan; KATO, Darryl; KIRSCHBERG, Thorsten, A.; LIU, Hongtao; LINK, John, O.; MITCHELL, Michael, L.; PARRISH, Jay, P.; SQUIRES, Neil; SUN, Jianyu; TAYLOR, James; BACON, Elizabeth, M.; CANALES, Eda; CHO, Aesop; KIM, Choung, U.; COTTELL, Jeromy, J.; DESAI, Manoj, C.; HALCOMB, Randall, L.; KRYGOWSKI, Evan, S.; LAZERWITH, Scott, E.; LIU, Qi; MACKMAN, Richard; PYUN, Hyung-Jung; SAUGIER, Joseph, H.; TRENKLE, James, D.; TSE, Winston, C.; VIVIAN, Randall, W.; SCHROEDER, Scott, D.; WATKINS, William, J.; XU, Lianhong; YANG, Zheng-Yu; KELLAR, Terry; SHENG, Xiaoning; CLARKE, Michael, O’Neil, Hanrahan; CHOU, Chien-hung; GRAUPE, Michael; JIN, Haolun; MCFADDEN, Ryan; MISH, Michael, R.; METOBO, Samuel, E.; PHILLIPS, Barton, W.; VENKATARAMANI, Chandrasekar; WO2010/132601; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics