Tag: M.W:200-300

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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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Piperazines – an overview | ScienceDirect Topics

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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3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To an aqueous (100 ml) sodium hydroxide (4.0 g, 100 mmol) solution of piperazine-2-carboxylic acid dihydrochloride (5 g, 24.63 mmol) is added a solution of di-tert-butyl dicarbonate (11.0 g, 50.45 mmol) in dioxan (50 ml) at 0 C. over a period of half an hour. The reaction mixture is stirred at 0 C. for 1 hr. followed by stirring at room temperature (25 C.) for another 2 hrs. Neutralized (pH 6-7) with aqueous 2N HCl, extracted with ethyl acetate. Organic layer washed with brine solution, dried (Na2SO4) and evaporated in vacuo to yield an oil which solidifies on cooling. (Yield 8.02 g, 98.76%).

3022-15-9, 3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TORRENT PHARMACEUTICALS LTD.; US2003/225102; (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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Acryloyl chloride (1.34 mL, 16.5 mmol) was added to a solution of (S)-1-boc-2-methyl-piperazine (3.00 g, 15.0 mmol, Boc Sciences, Shirley, N.Y.) in THF (30.0 mL) at -10 C., and the resulting mixture was stirred at -10 C. for 5 min. Triethylamine (6.26 mL, 44.9 mmol) was then slowly added, and the resulting mixture was stirred at -10 C. for 15 min, then allowed to warm to rt. The reaction mixture was partitioned between EtOAc and saturated aqueous NaHCO3. The aqueous layer was extracted with EtOAc (3¡Á), and the organic layers were then combined, dried over MgSO4, filtered, and concentrated in vacuo. Chromatographic purification of the residue (silica gel, 0-100% EtOAc in heptane) furnished (S)-tert-butyl 4-acryloyl-2-methylpiperazine-1-carboxylate: 1H NMR (400 MHz, DMSO-d6) delta 6.72-6.85 (m, 1H) 6.10-6.18 (m, 1H) 5.68-5.76 (m, 1H) 4.08-4.32 (m, 2H) 3.68-4.03 (m, 2H) 2.86-3.14 (m, 2H) 2.66-2.80 (m, 1H) 1.38-1.43 (s, 9H) 0.96-1.04 (m, 3H). m/z (ESI, +ve) 277.3 (M+Na)+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Amgen Inc.; LANMAN, Brian Alan; CHEN, Jian; REED, Anthony B.; CEE, Victor J.; LIU, Longbin; KOPECKY, David John; LOPEZ, Patricia; WURZ, Ryan Paul; NGUYEN, Thomas T.; BOOKER, Shon; NISHIMURA, Nobuko; SHIN, Youngsook; TAMAYO, Nuria A.; ALLEN, John Gordon; ALLEN, Jennifer Rebecca; (266 pag.)US2018/334454; (2018); A1;,
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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.

Intermediate 3 (2.63 g, 13.1 mmol) was dissolved in DCE (60 mL). Cyclobutanone (1.38 g, 19.7 mmol) and acetic acid (0.75 mL, 13.1 mmol) were added and the mixture stirred at rt for 30 min. NaBH(OAc)3 (4.18 g, 19.7 mmol) was added portionwise and the mixture was stirred at rt overnight. Sat. Na2CO3 (50 mL) was added and the aq. layer was extracted with DCM (3¡Á75 mL). The combined organic phases were dried over Na2SO4, filtered and concentrated under reduced pressure to provide 2.58 g title compound (77%) as an oil. 1H NMR (300 MHz, CDCl3) delta ppm 0.97 (d, J=6.4 Hz, 3H) 1.45 (s, 9H) 1.61-1.70 (m, 2H) 1.81-1.91 (m, 1H) 1.93-2.00 (m, 2H) 2.03-2.14 (m, 2H) 2.41-2.51 (m, 1H) 2.58-2.65 (m, 1H) 2.94-3.05 (m, 1H) 3.06-3.16 (m, 1H) 3.29-3.58 (m, 3H).

163765-44-4, The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; US2010/216812; (2010); 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.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

General procedure: An aqueous solution of sodium bicarbonate (0.57g, 6.78mmol) (20mL) was stirred at r.t. for 10min, and then compound 5a (0.50g, 2.26mmol) in dichloromethane (10mL) was added under ice-cooling. Thiophosgene (0.39g, 3.39mmol) in dichloromethane solution (5mL) was added dropwise for 0.5h. Reaction was stirred under ice-cooling for 6h. The aqueous phase was extracted with dichloromethane (20mL¡Á3). The combined organic phase was washed twice with saturated brine (20mL¡Á2) and dried over anhydrous MgSO4. After filtration, the solvent of filtrate was removed in vacuo, and the residue was purified by silica gel column chromatography (DCM : MeOH=100 : 1) to afford compound 6a as a pale-yellow solid; Yield: 63%, 55121-99-8

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Heng, Hao; Wang, Zhijie; Li, Hongmei; Huang, Yatian; Lan, Qingyuan; Guo, Xiaoxing; Zhang, Liang; Zhi, Yanle; Cai, Jiongheng; Qin, Tianren; Xiang, Li; Wang, Shuxian; Chen, Yadong; Lu, Tao; Lu, Shuai; European Journal of Medicinal Chemistry; vol. 176; (2019); p. 248 – 267;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A previously described method [19] was followed for the syntheses of 1-5, 7, 8, 10 and 20. Briefly, equimolar quantities of the amine and the acridine/quinoline were dissolved in ethanol, 2 drops of conc. HCl were added and the mixture refluxed for ca 24 h. On cooling, NaOH (1 M) or ammonia solution (25%) was added, followed by dichloromethane to extract the product. Alternatively, if the product precipitated out of solution on alkalinization, it was removed by filtration and purified by column chromatography.

115619-01-7, 115619-01-7 4-(4-Ethylpiperazin-1-yl)phenylamine 936738, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 2917 – 2929;,
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.55083-85-7,1-(4-Chlorophenyl)piperazin-2-one,as a common compound, the synthetic route is as follows.,55083-85-7

4-Methoxy-3-(pyridin-2-ylethynyl)benzoic acid (51 mg, 0.2 mmol), 1-(4- chlorophenyl)piperazin-2-one (74 mg, 0.3 mmol), and triethylamine (105 uL, 0.75 mmol) were dissolved in 3 ml. of CH2CI2 and treated with HOBt (34 mg, 0.25 mmol) and EDC (48 mg, 0.25 mmol). The reaction was stirred at room temperature overnight and directly purified by flash chromatography on silica gel (CH2CI2/Et0Ac) to yield 85 mg (95%) of the product as a white solid.

The synthetic route of 55083-85-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; WYETH; WO2009/143404; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics