Month: May 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

154590-35-9, Step 4: To the product of Step 3 (0.63 g, 2.1 mmol) in CH2Cl2 (10 ml) add DIPEA (0.56 ml, 3.2 mmol), followed by AcCl (0.18 ml, 2.6 mmol). Stir 0.5 h, concentrate, and purify by PLC to obtain the amide as a brown oil

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Schering Corporation; US2004/220194; (2004); A1;,
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

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A:(3R)-tert-butyl 4-(2-(3-cyano-2,4-difluorophenyl):-2-hydroxyethyl)-3-(hydroxYmethyl)piperazine-1-carboxylateate; 2,6-difluoro-3-( oxiran-2-yl)benzonitrile (3. 70 g, 20.4mmol) and (R)-tert-butyl3-(hydroxymethyl)piperazine-1-carboxylate (6.63 g, 30.6 mmol) weredissolved in ethanol (36.0 mL) then placed in 3-20mL sealed tubes and microwaved at 140C for 1 h. The solvents were evaporated and the combined residue was purified by chromatographythrough a 120g ISCO Redi-sep column with 50% to 100% ethyl acetate/hexane solvent system toyield the title compound LC-MS (IE, m/z): 398 [M +1]+., 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; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); 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.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

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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 14; l-Methyl-2-[(2R)-2-methyl-4-(quinoline-2-carbonyl)-piperazin-l-yl]- 1eta- [4,4′]bipyrimidinyl-6-one; (3R)-3’Methvl-4′(l-methvl’6-oxo-l,6-dihvdro-[4,4′]bipvrimidinvl-2’vl)-piperazine-l’car boxvlic acid tert-butvl ester; A solution of 2-chloro-3-methyl-6-(pyrimidin-4-yl)-3H-pyrimidin-4-one (5.3 g, 24 mmol), fer^butyl (Si^-S-methylpiperazine-l-carboxylate (5.0 g, 25 mmol) and triethylamine (7.6 g, 75 mmol) in N-methyl”2-pyrrolidone (25 ml) was stirred for 6 hours at 90 0C. The solution was partitioned between water and ethyl acetate, and the organic layer was washed with water, brine, dried over sodium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (eluent; ethyl acetate) to afford (3R)-3-methyl-4-(l-methyl-6-oxo-l,6- dihydro-[4,4′]bipyrimidinyl-2-yl)-piperazine”l-carboxylic acid tert-butyl ester (6.9 g, 71 %)..1H NMR; 1.28 (3H, d, J= 7.0 Hz), 1.51 (9H, brs), 3.29-3.52 (4H, m), 3.55 (3H, s), 3.71 (IH, dd, J= 3.9, 13.3 Hz), 3.81-4.02 (2H, m), 7.29 (IH, s), 8.16 (IH, dd, J= 1.6, 5.5 Hz), 8.88 (IH, d, J= 4.7 Hz), 9.25 (IH, s) (CDCl3) MS; [M++ 1] = 387 ., 163765-44-4

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

Reference：
Patent; MITSUBISHI PHARMA CORPORATION; SANOFI-AVENTIS; WO2007/119463; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112257-12-2, tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 4-(2-bromo- acetyl)-piperazine-l-carboxylic acid tert-butyl ester (0.39 g, 1.3 mmol) and 2-nitro-6,7- dihydro-5H-imidazo[2,l-b][l,3]oxazin-6.Sr-ol (0.2 g, 1.08 mmol) in DMF (9 ml) was cooled to -60 0C and treated with sodium hydride (50 mg, 1.3 mmol) and warmed to room temperature over 2 h. The mixture was diluted with ethyl acetate, washed with water dried over sodium sulfate and concentrated. The residue is purified by silica gel chromatography (5% methanol in dichloromethane) to give 4-[2-(2-nit?>-6,7-dihydro-5H- imidazo[2,l-b][l,3]oxazin-6S-yloxy)-acetyl]-piperazine-l-carboxylic acid tert-butyl ester as a yellow oil (314 mg, 77%). ESI MS m/z 434 (M + Na+); 1H NMR (400 MHz, CDCl3) delta 7.48 (s, IH), 4.48-4.40 (m, IH), 4.40-4.22 (m, 4H), 3.38-3.44 (s, 2H), 3.42-3.30 (m, 8H), 1.42 (s, 9H)., 112257-12-2

The synthetic route of 112257-12-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CUMBRE PHARMACEUTICALS INC.; WO2008/8480; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

438049-35-5, N-Boc-3-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1, 1′-carbonyldiimidazole (468 mg, 2.80 mmol) in anhydrous DMF (2 mL) were added triethylamine (0.59 mL, 4.20 mmol) and a solution of tert-butyl 3-ethylpiperazine-1-carboxylate (500 mg, 2.33 mmol) in anhydrous DMF (2 mL) dropwise. The mixture was stirred in a sealing tube at rt for 30 min, and then anhydrous methanol (12 mL) was added. The resulting mixture was further stirred at 60 for 24 h, and concentrated. The residue was diluted with saturated aqueous NaCl (30 mL) , and extracted with EtOAc (15 mL × 2) . The combined organic layers were dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 5/1 to give 4-tert-butyl 1-methyl 2-ethylpiperazine-1, 4-dicarboxylate as colorless liquid (260 mg, 40) .1H NMR (400 MHz, CDCl3) : delta ppm 3.88-3.97 (m, 4H) , 3.70 (s, 3H) , 2.76-3.02 (m, 3H) , 1.52-1.61 (m, 2H) , 1.45 (s, 9H) , 0.89 (t, J 7.4 Hz, 3H) and MS-ESI: m/z 173.1 [M+H-100] + ., 438049-35-5

438049-35-5 N-Boc-3-Ethylpiperazine 22219867, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (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

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

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