Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, b) 4-(5-Trifluoromethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl esterTo 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%).; a) 4-(5-Hydroxymethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl esterTo a solution of 179 mmol 30% aqueous hydrogen peroxide in 60 ml water was added 1 N aqueous sodium hydroxide solution until the pH was 9. The reaction mixture was then cooled to 100C and 163 mmol acrolein was added dropwise. Further amounts of 1 N aqueous sodium hydroxide solution were added during the addition in order to maintain the pH of the reaction mixture between pH 8 and 9. The mixture was stirred for 30 min at 0 0C and then 40.8 mmol thiocarbamoyl-piperazine-1-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) was added. To the resulting suspension was added 25 ml ethanol and the mixture was heated at 80 0C for 30 min. The resulting solution was diluted with ethyl acetate/tetrahydrofuran (1:1) and the mixture was washed twice with brine. The organic phase was dried over sodium sulphate and concentrated in vacuo to afford the title compound as a yellow oil (yield 99%). MS (m/e): 300.3 (M+H+, 100%).;f) 4-(4-Methyl-5-trifluoromethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl esterA mixture of 4.92 mmol rac-2-benzenesulfonyl-2-methyl-3-trifluoromethyl- oxirane and 5.41 mmol 4-thiocarbamoyl-piperazine-l-carboxylic acid tert-butyl ester (prepared from tert-butyl 1-piperazinecarboxylate, l.l’-thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054) in 15 ml N,N-dimethylformamide was heated at 100 0C for 4.5 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 a yellow crystalline solid (yield 30%). MS (m/e): 352.3 (M+H+, 100%).; a) 4-(Dimethylaminomethylene-thiocarbamoyl)-piperazine-l-carboxylic acid tert-butyl esterA mixture of 122 mmol N,N-dirnethylformamide dimethyl acetal and 6.11 mmol 4- thiocarbamoyl-piperazine-1-carboxylic acid tert-butyl ester (prepared from tert-butyl 1- piperazinecarboxylate, lj’-thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054) was heated at 110 0C for 3 h. The reaction mixture was then concentrated in vacuo and the residue was resuspended in ethyl acetate/ tetrahydrofuran ( 1:1) and washed with brine. The organic phase was dried over sodium sulphate and concentrated in vacuo to afford the title compound as a light yellow crystalline solid (yield 95%). MS (m/e): 301.4 (M+H+, 100%).

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; WO2006/72436; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

(a) 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (Compound A)2-Fluoro-5-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]benzoic acid (D)(15.23g, 51.07 mmol) was suspended with stirring under nitrogen in acetonitrile (96 ml). Diisopropylethylamine (19.6 ml, 112.3 mmol) was added followed by 1-cyclopropylcarbonylpiperazine (l)(9.45g, 61.28 mmol) and acetonitrile (1ml). The reaction mixture was cooled to 18C. O-Benzotriazol-1-yl- tetramethyluronium hexafluorophosphate (25.18g, 66.39 mmol) was added over 30 minutes and the reaction mixture was stirred for 2 hours at room temperature. The reaction mixture was cooled to 3C and maintained at this temperature for 1 hour, before being filtered. The filter cake was washed with cold (3C) acetonitrile (20 ml) before being dried in vacuo at up to 400C to give the title compound as a pale yellow solid (20.21 g).Mass Spectrum: MH+ 4351H NMR (400MHz, DMSO-d6) delta: 0.70 (m, 4H), 1.88 (br s, 1H), 3.20 (br s, 2H), 3.56 (m, 6H), 4.31 (s, 2H), 7.17 (t, 1H), 7.34 (dd, 1 H), 7.41 (m, 1H), 7.77 (dt, 1H), 7.83 (dt, 1H), 7.92 (d, 1H), 8.25 (dd, 1 H)1 12.53 (S1 1H).

59878-57-8, The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; KUDOS PHARMACEUTICALS LIMITED; WO2009/50469; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Method 25 1-Acetyl-4- piperazine; 1-Butyl-3-methylimidazolium tetrafluoroborate (1.75g, 7. 74mmol) was added to a stirred solution of l-fluoro-2-methyl-4-nitrobenzene (12g, 77. 35mmol) and 1-acetylpiperazine (39.7g, 309. 4mmol) in acetonitrile (3ml). The reaction mixture was then heating at 95C overnight. The reaction mixture was allowed to cool down to room temperature. The solution was diluted with EtOAc and water. The precipitate formed was filtered off to give a solid corresponding to the required product. The organics were washed with water (4 times), brine, dried and evaporation of solvent to give a solid. Both solids were combined and after trituration with isohexane/ether and filtration, the title compound was obtained as a yellow solid which was dried in vac oven overnight at 50C. (19. 61g, 96%). NMR (400MHz) 2.06 (s, 3H), 2.38 (s, 3H), 2.99 (dt, 4H), 3.61 (m, 4H), 7.14 (d, 1H), 8.04 (dd, 1H), 8.07 (d, 1H); m/z 264., 13889-98-0

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/75461; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

75336-86-6, (R)-2-methylpiperazine (1.25g, 12.5mmol), and K2CO3 (4.0g) were combined with chloroform (30 mL) in a 50mL flask fitted with a magnetic stirrer. A chloroform (25 mL) solution of 1-chloromethyl-4-vinylbenzene (4.00 g, 26.2 mmol) was added dropwise slowly within 30min at 40-50 °C under stirring. The reaction mixture was heated to reflux for 4h till the starting material disappeared by TLC detection (n-hexane:ethyl acetate=5:1, V/V). The resultant mixture was filtered to remove the solid. The solvent was removed from the filtrate under reduced pressure to yield a viscous oil that was then diluted with ethanol (60mL). Adding HCl/ethanol to the above solution till pH 1-2 yielded a white solid. The resultant precipitate was collected by suction filtration, washed with cold ethanol, and then mixed with water (10mL). The pasty was adjusted to pH 10-11 with ammonium hydroxide and then extracted with methylene dichloride twice (80 mL). The organic phase was washed with saturated brine and dried with magnesium sulfate. Removing solvent afforded 3.3 g (R)-MbVBP as white crystalline powders in 79.5percent yield based on (R)-2-methylpiperazine.

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Wang, Guo-Xi; Xing, Zheng; Chen, Li-Zhuang; Han, Guang-Fan; Journal of Molecular Structure; vol. 1091; (2015); p. 16 – 19;,
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.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

115761-79-0, General procedure: To a solution of 4 (100 mg, 0.23 mmol) in acetonitrile (CH3CN, 10 mL) was added the corresponding arylpiperazine or phenylpiperidine (1.2 equiv) and potassium carbonate (6.0 equiv). The reaction mixture was stirred at reflux for 16 h. After cooling to ambient temperature, the reaction mixture was filtered through a Buchner funnel. After filtration the filtrate was concentrated in vacuo and the residue was purified by silica gel column chromatography using ethyl acetate/petroleum ether (1/5, v/v) as eluent to afford the corresponding products, and all compounds were recrystallized from trichloromethane and n-hexane.

As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference：
Article; Chen, Hong; Liang, Xue; Xu, Fang; Xu, Bingbing; He, Xuelan; Huang, Biyun; Yuan, Mu; Molecules; vol. 19; 8; (2014); p. 12048 – 12064;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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,934-98-5

A mixture of (S)-isopropyl 2-(tert-butoxy)-2-(4-(4,4-dimethylpiperidin-1-yl)-S -(4-(4-fluorophenethoxy)phenyl)-2-methyl-6-(((trifluoromethyl)sulfonyl)oxy)pyridin-3 -yl)acetate (0.02 g, 0.027 mmol) and 2-(4-methylpiperazin-1-yl)ethanamine (0.0 16 g,0.108 mmol) in NMP (1 mL) was heated at 180 °C for 2 h. Ethanol (0.5 mL) and 5 MNaOH (0.054 mL, 0.271 mmol) were added and the mixture was heated at 80 °C for 4.5cooled to ambient temperature, and filtered. The cmde mixture was purified viapreparative HPLC to afford the desired product (11.8 mg, 62percent). LCMS (M+1) = 690.2.

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

Reference：
Patent; VIIV HEALTHCARE UK (NO.5) LIMITED; BELEMA, Makonen; BOWSHER, Michael S.; DESKUS, Jeffrey A; EASTMAN, Kyle J.; GILLIS, Eric P; FRENNESSON, David B; IWUAGWU, Christiana; KADOW, John F.; NAIDU, B. Narasimhulu; PARCELLA, Kyle E.; PEESE, Kevin M; SAULNIER, Mark G; SIVAPRAKASAM, Prasanna; (463 pag.)WO2018/127800; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,74879-18-8

In a sealed tube, 7-fluoro-2-(2-methyl-[l,2,4]triazolo[l,5-a]pyrimidin-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one (Intermediate (VT1), 30 mg, 0.101 mmol), (S)-2-methylpiperazine (30.4 mg, 0.304 mmol, 3 eq.) and TEA (51.2 mg, 70.6 mu, 0.506 mmol, 5 eq.) were dissolved in DMSO (2 ml). The reaction mixture was heated at 120 C for 12 hours. The crude was filtered to afford the title product (29 mg, 77%) as a yellow solid. MS m/z 377.2 [M+H]+.

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

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; GILLESPIE, Robert Jack; HASANE, Ratni; SARIE, Jerome Charles; (89 pag.)WO2016/184832; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: In the nitrogen atmosphere of the glove box, 3.33 mg of ruthenium complex 1c was dissolved in 50 mL of tetrahydrofuran. After stirring, a catalyst 1c stock solution was formed. 1 ml of the above solution was added to a 125-mL Parr autoclave (0.067 mg, 0.0001 mmol). 1c), And added 9mL of tetrahydrofuran, Morpholine (8.712 g, 100 mmol). After the autoclave is sealed, it is taken out of the glove box. The carbon dioxide gas and hydrogen gas were each charged at 40 atm. The reaction system is heated to 120 C in an oil bath. The pressure rises to about 120 atm, After stirring for 181 hours, The reactor was then cooled to room temperature in a water bath. Slowly release the remaining gas in the fume hood, A pale yellow liquid was obtained. P-xylene (200 muL) was added to the mixture as an internal standard. The yield of N-formylmorpholine was determined by gas chromatography to be 94%.

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference：
Patent; Chinese Academy Of Sciences Shanghai Organic Chemistry Institute; Ding Kuiling; Qiu Jia; Yan Tao; Zhang Lei; Wang Zheng; (49 pag.)CN109553641; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55276-43-2, 1-Methanesulfonylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55276-43-2, A mixture of 2-biphenylylcyanamide (3.8 g), 1-methanesulphonylpiperazine (3.8 g) and ethanol (60 ml) was heated at 90-95 C. for 12 hours to give N-(2-biphenylyl)-4-methanesulphonylpiperazine-1-carboxamidine (m.p. 178-180 C.) which was recrystallized from ethanol.

55276-43-2 1-Methanesulfonylpiperazine 709161, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; The Boots Company; US5302720; (1994); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics