Heterocyclic Building Blocks-piperazine

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;,
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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;,
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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;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.197638-83-8,1-Boc-4-(4-Formylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: The startingcompound 3-(cyanoacetyl)indole was prepared according tothe procedure described by Slatt et al. [66].A mixture of 3-(cyanoacetyl)indole (1mmol) andheteroaryl-aldehydes a-i (1mmol) in ethanol 0.5mL wasirradiated at 300W and 100C for 8-90min, respectively.After completion of the reaction, the mixture was allowedto cool to room temperature and collected by filtration.The solid products were isolated by crystallization of thereaction mixture from ethanol and washed with a coolmixture of hexane/ethanol (7 : 3, 3 ¡Á 4 mL) to give thecorresponding compounds.The solid products obtainedwerepurified by flash column chromatography performed withSilica gel (60-120mesh) and/or recrystallization using amixture of petroleum ether and ethyl acetate (7 : 3 and 6 : 4)or dichloromethane (CH2Cl2) as

197638-83-8, 197638-83-8 1-Boc-4-(4-Formylphenyl)piperazine 2795509, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Treuer, Adriana V.; De-La-Torre, Pedro; Gutierrez, Margarita I.; Journal of Chemistry; vol. 2017; (2017);,
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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

Intermediate 2 (5 mmol),1-tert-butoxycarbonylpiperazine (6 mmol) and DIEA (7.5 mmol) were dissolved in 5 ml of dioxane, and microwaved at 80 C for 2 h. The solvent was evaporated under reduced pressure, and the mixture was evaporated, evaporated, evaporated, evaporated, evaporated, Recrystallization gave Intermediate 3. White solid, the yield is 78.5%.

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; Shandong University; Zhao Guisen; Yu Shengping; Liu Yang; Wang Luhua; Guo Kaiwen; Hou Xianxin; (33 pag.)CN108997351; (2018); A;,
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623586-00-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.623586-00-5,(R)-1-Cbz-3-methylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of (2 ,5 )-tert-butyl 5-(chloromethyl)-4-(2-(6-(4-fluorobenzyl)-3,3-dimethyl-2,3- dihydro-lH-pyrrolo[3,2-b]pyridin-l-yl)-2-oxoethyl)-2-methylpiperazine-l-carboxylate ( 8.67 g, 15.91 mmol, obtained as described in WO 2012/143726) in acetonitrile (50.0 mL) and was added (R)- benzyl 3-methylpiperazine-l-carboxylate (4.10 g, 17.50 mmol, commercially available from, for example, Fluorochem), sodium iodide (0.238 g, 1.591 mmol) and potassium carbonate (6.59 g, 47.7 mmol) and the reaction was stirred at 80 C for 18 hours. The volatiles were removed in vacuo, the reaction was diluted in 100 mL DCM and was washed with 100 mL saturated sodium bicarbonate solution and 100 mL water. The aqueous layer was washed with an additional 2 x 100 mL DCM, and the combined organic layers were washed with 100 mL brine and passed through a Biotage phase separator. The volatiles were removed in vacuo. The residue was dissolved in 25 mL DCM and loaded onto 340g KP-Sil SNAP cartridge and purified by flash chromatography: 2% methanol in DCM for lcolumn volume, 10 column volumes gradient 2% to 12% methanol in DCM and 2 column volumes 12% methanol in DCM. Compound eluted at 7 column volumes to afford the title compound (9.26 g, 12.5 mmol, 78 % yield). LCMS RT= 1.05 min, ES+ve 743.

As the paragraph descriping shows that 623586-00-5 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; CASILLAS, Linda N.; HARLING, John David; MIAH, Afjal Hussain; SMITH, Ian Edward David; RACKHAM, Mark David; (204 pag.)WO2017/182418; (2017); A1;,
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692058-21-2, 1-Boc-4-(2,2,2-trifluoroethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,692058-21-2

2-(lH-Indazol-4-yl)-4-mophiholin-4-yl-6-[4-(2,2,2-trifluoro-ethyl’)-piperazin-l- ylmethyl]-thieno[3,2-dlpyrimidine (90).Prepared via 2-Chloro-4-morpholin-4-yl-6-[4-(2,2,2-trifluoro-ethyl)- piperazin-l-ylmethyl]-thieno[3,2-d]pyrimidine, prepared from l-(2,2,2-trifluoro- ethyl)-piperazine.Amine preparation: to BOC-piperazine (4g) in DCM (4OmL) was added trifluoroacetic anhydride (6.06mL) and triethylamine (3.29mL). After stirring overnight the reaction mixture was diluted with diluted with DCM, washed with sodium bicarbonate solution, dried (MgSO4) and the solvent removed in vacuo to yield 4-(2,2,2-trifluoro-acetyl)-piperazine-l-carboxylic acid tert-butyl ester (6.06g).To 4-(2,2,2-trifluoro-acetyl)-piperazine-l-carboxylic acid tert-butyl ester (6.06g) in dry THF (6OmL) was added borane dimethyl sulfide complex (4.5ml) and EPO the reaction mixture was heated to reflux. After 2 h the reaction mixture was cooled to O0C and MeOH was carefully added, followed by water. The organics were extracted into ethyl acetate, dried (MgSO4) and the solvent removed in vacuo to yield 4-(2,2,2-trifluoro-ethyl)-piperazine-l-carboxylic acid tert-butyl ester (4.46g). Treatment with HCl in DCM/MeOH yielded the desired compound, which was isolated as the hydrochloride salt.1H NMR (400MHz, CDCl3): 2.56 (4H, m), 2.69 (4H, m), 2.93 (2H, q), 3.79 (2H, s), 3.85 (4H, m), 4.02 (4H, m), 7.23 (IH, s), 7.44 (IH, d), 7.52 (IH, d), 8.21 (IH, d), 8.94 (IH, s).

692058-21-2 1-Boc-4-(2,2,2-trifluoroethyl)piperazine 16748694, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PIRAMED LIMITED; WO2006/46031; (2006); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of 3-bromobiphenyl (300 mg, 1.28 mmol), 1-cyclopentylpiperazine (238 mg, 1.54 mmol), sodium tert.-butoxide (173 mg, 1.8 mmol), tris(dibenzylideneacetone)dipalladium (12 mg, 0.01 mmol) and racemic 2,2′-bis(diphenylphosphino)-1,1’binaphthyl (24 mg, 0.04 mmol) in toluene (11 ml) was mixed under nitrogen in a closed reaction vessel. The reaction mixture was stirred at 80 C. for 3 days in a closed reaction vessel. It was cooled to room temperature and washed with water (2¡Á10 ml). The combined organic layers were extracted with 1 N hydrochloric acid (2¡Á20 ml). The combined aqueous extracts were made basic with an 1 N aqueous sodium hydroxide solution and extracted with tert-butyl methyl ether (3¡Á20 ml). The tert-butyl methyl ether layers were dried over magnesium sulphate. The solvent was removed in vacuo to give 220 mg of the title compound. [0919] 1H-NMR (CDCl3, two sets of signals, broad signals) delta1.35-1.85 (m, 6 H); 1.95 (m, 2 H); 2.55 (m, 1 H); 2.70 (m, 4 H); 3.30 (m, 4 H); 6.95 (d, 1 H); 7.05 (d, 1 H); 7.15 (s, 1 H); 7.35 (t, 2 H); 7.45 (t, 2 H); 7.60 (d, 2 H). HPLC method B: elution at 10.45 min. [0920] The title compound was transferred into its hydrochloride salt, by dissolving it in ethyl acetate (5 ml). A 3.2 M solution of hydrogen chloride in ethyl acetate (5 ml) was added. The solvent was removed in vacuo. The residue was dissolved in ethanol (50 ml). The solvent was removed in vacuo., 21043-40-3

21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Hohlweg, Rolf; Dorwald, Florencio Zaragoza; Stephensen, Henrik; Pettersson, Ingrid; Peschke, Bernd; US2003/236259; (2003); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

mCPBA (<77% pure) (15.5 mg, assumed 0.069 mmol) in DCM (0.5 mL) was added to a stirred solution of 6 - (2 -chloropyridin-3 -yl ) -2 - (methylthio) pyrido [4 , 3 -d] pyrimidin-5 (6H) -one (18.2 mg, 0.060 mmol) in toluene (1.5 mL) at RT under nitrogen. After 15 min, DIPEA (0.031 mL, 0.179 mmol) and tert-butyl 4- (4- aminophenyl) piperazine-l-carboxylate (18.2 mg, 0.066 mmol) [commercially available] were added, successively, and thetemperature was increased to 60 C. After 16 h, the reaction mixture was allowed to cool to RT, and was loaded onto a KP-NH column and purified by flash chromatography (0- 100%, EtOAc in cyclohexane) to give the title compound (14.3 mg, 45%) as a yellow solid. LCMS (Method A) : RT = 1.33 min, m/z = 534 [M+H]+., 170911-92-9

170911-92-9 tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate 11011301, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ALMAC DISCOVERY LIMITED; O’DOWD, Colin Roderick; ROUNTREE, James Samuel Shane; BURKAMP, Frank; WILKINSON, Andrew John; WO2014/167347; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-31-7,1-Ethylpiperazine-2,3-dione,as a common compound, the synthetic route is as follows.

59702-31-7, 1) taking N-ethyldioxypiperazine 14.2 g (0.10 mol),Transfer to a 500 mL three-necked flask, stir, and add 200 mL of dichloromethane.Cool down to -25 to -20 C, add 16.3 g (0.15 mol) TMCS,Control temperature -25 ~ -20 C, add 11.9g (0.15mol) pyridine,Adding 0.018 g of DMAP, adding 11.9 g (0.04 mol) of triphosgene in batches at a temperature of -25 to -20 C, and maintaining the reaction for 30-60 minutes;After the reaction was completed, suction filtration, washing with 30 mL of dichloromethane and distillation to dryness under reduced pressure.Add 100 mL of n-hexane to crystallize and filter by suction.Drying gave 19.3 g of N-ethylbisoxypiperazine chloride in a yield of 94.3%.

59702-31-7 1-Ethylpiperazine-2,3-dione 108812, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Qilu Tianhe Huishi (Leling) Pharmaceutical Co., Ltd.; Qilu Tianhe Huishi Pharmaceutical Co., Ltd.; Sun Zhengjun; Fan Changying; Sun Yue; Li Yong; (7 pag.)CN109734725; (2019); A;,
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