Month: August 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2815-34-1,trans-2,5-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Diisopropylethylamine (0.38 ml) was added to a solution of tra?is-2,5-dimethyl- piperazine (1.50 g), phenyl acetic acid (0.59 g) and HATU (1.55 g) in DMF (10 ml). The reaction mixture was stirred overnight at ambient temperature. The solution was diluted with water, then extracted with ethyl acetate. The organic extracts were dried (MgSO4) then concentrated in vacuo to give the sub-title compound (1.8 g). EPO MS: APCI (+ve): 233 (M+l)

2815-34-1, 2815-34-1 trans-2,5-Dimethylpiperazine 220672, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/56752; (2006); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step A: (S)-tert-butyl 4-((S)-2-hydroxy-2-( 4-methyl-1-oxo-1 ,3-dihydroisobenzofuran-5-yl)ethyl)-3-(hydroxymethyl)piperazine-1-carboxylate: (S)-4-Methyl-5-( oxiran-2-yl)isobenzofuran-1 (3H)one(0.75g, 3.95 mmol) and (S)-tert-butyl3-(hydroxymethyl)piperazine-1-carboxylate (1.02 g,4.73 mmol) in ethanol (12 mL) were heated in microwave at 150 oc for 1.5 h. The reaction solution was concentrated and the residue was purified by MPLC on a Biotage system using 40-100% ethyl acetate/hexane to give the title compound. LC/MS: (M+1)+: 407.15., 314741-40-7

As the paragraph descriping shows that 314741-40-7 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

55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The mixture of B (10.92g, 20.0mmol)), HATU (9.12g, 24.0mmol) and DIEA (3.87g, 30.0mmol) in DMF (lOOmL) was stirred at room temperature for 0.5h, then was added la (5.26g, 24.0mmol). The resulting mixture was stirred at room temperature for 0.5h and evaporated. The residue was purified by columnchromatography (EA:MeOH=5:l) to provide lb (12.43g, 83.2%)., 55121-99-8

55121-99-8 (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone 231408, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; XCOVERY HOLDING COMPANY, LLC; LIANG, Congxin; WO2012/48259; (2012); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

639068-43-2, tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

639068-43-2, Referential Example 88]; 3,4,5-Trimethylpiperazine-1-carboxylic acid tert-butyl ester ; 3,5-Dimethylpiperazine-1-carboxylic acid tert-butyl ester (3.31 g) obtained from Referential Example 87 was dissolved in methanol (50 mL). To the resultant solution, 10percent palladium-carbon (0.504 g), 35percent aqueous formalin (1.85 mL), and 1M HCl in ethanol (15.4 mL) were added at room temperature, and the mixture was stirred in a hydrogen atmosphere for 19 hours. 10percent Palladium-carbon (0.95 g), 35percent aqueous formalin (1.8 mL), and 1M HCl-ethanol (15 mL) were added thereto, followed by stirring in a hydrogen atmosphere for 23 hours. After the system was purged with nitrogen, the resultant mixture was neutralized through addition of the aqueous sodium hydroxide, and insoluble matter was removed by filtration. The filtrate was brought to dryness under reduced pressure. The residue was purified through silica gel column chromatography (chloroform – 7N ammonia/methanol), to thereby give the title compound as an oily product (2.28 g, 65percent).1H-NMR(400MHz,CDCl3)delta: 1.08(6H,d,J=6.1Hz), 1.45(9H,s), 2.00-2.20(2H,m), 2.25(3H,s), 2.60(2H,br), 3.85(2H,br). MS(FAB)m/z: 229(M+H)+.

The synthetic route of 639068-43-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1591443; (2005); 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.

EXAMPLE 14 7-(2-(4-(2,4-Difluorophenyl)piperazin-1-yl)propyl)-2-(furan-2-yl)-7H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, Method A To a suspension of NaH (13.0 mg, 60 wt % in mineral oil, 0.3 mmol) in 2.0 mL of anhydrous DMF is added 2,4-difluorophenylpiperazine (63 mg, 0.32 mmol). After stirring the solution at RT for 15 min, a solution of 1-(5-amino-2-(furan-2-yl)-7H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-7-yl)propan-2-yl methanesulfonate (80 mg, 0.21 mmol) in 1.5 mL of anhydrous DMF is added. The reaction is stirred at RT under N2 for 12 h. However, very little of product formation is seen by LC/MS. The reaction is then heated at 100 C. for 12 h to complete the reaction as detected by LC/MS. The crude reaction mixture is purified by chromatography to afford 7-(2-(4-(2,4-difluorophenyl)piperazin-1-yl)propyl)-2-(furan-2-yl)-7H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine: 1H NMR (400 MHz, CD2Cl2) delta 1.05 (d, 3H, J=6.83 Hz), 2.62-272 (m, 2H), 2.83-3.05 (m, 8H), 3.13-3.22 (m, 1H), 4.10 (dd, 1H, J=14.06 Hz and 6.64 Hz), 4.27 (dd, 1H, J=13.96 Hz and 7.52 Hz), 6.61 (dd, 1H, J=3.51 Hz and 1.76 Hz), 6.73 (d, 1H, J=3.51 Hz), 6.76-6.96 (m, 4H), 7.00 (d, 1H, J=3.32 Hz), 7.22 (dd, 1H, J=3.51 Hz and 0.78 Hz), 7.63 (dd, 1H, J=1.76 HZ and 0.78 Hz)., 115761-79-0

The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Moorman, Allan R.; US2008/242672; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

187669-60-9, 1-(4-(Methylsulfonyl)phenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 81; 4-{2-[4-(4-Mcthancsulfonylphcnyl)pipcrazin-l-yl]-2-oxocthyl}pipcridinc-l- carboxylic acid tert-butyl ester; To a solution of 4-hydroxy-4-(3-hydroxypropyl)piperidine-l-carboxylic acid tert-butyl ester (1.00 g, 3.86 mmol) in DCM (60 mL) was added Dess-Martin periodinane (1.80 g, 4.24 mmol) and the mixture was stirred for Ih at rt, a further batch of Dess-Martin periodinane (0.20 g, 0.47 mmol). The reaction mixture was quenched with 2 M NaOH and extracted with Et2O, the aqueous phase was re-extracted with Et2O and the organic extracts were combined then washed with water, 2 M NaOH solution and brine, dried (MgSO4) and the solvent was removed under vacuum to give 2-hydroxy-l-oxa-8-azaspiro[4.5]decane-8-carboxylic acid tert-butyl ester. A solution of l-(4-methanesulfonylphenyl)piperazine (0.12 g, 0.50 mmol) and 2-hydroxy-l-oxa- 8-azaspiro[4.5]decane-8-carboxylic acid tert-butyl ester (0.14 g, 0.56 mmol) in anhydrous MeOH (2 mL) was heated at 750C for Ih, then NaBH4 (25 mg, 0.65 mmol) was added and the reaction was stirred for 2h. The solvent was removed under vacuum and the resulting residue was partitioned between water and DCM. The aqueous phase was re-extracted with DCM, the EPO organic extracts were combined and purified by flash chromatography eluting with 3:97 MeOH:DCM to afford the title compound: RT = 2.37 min; m/z (ES+) = 482.45 [M+H]+., 187669-60-9

187669-60-9 1-(4-(Methylsulfonyl)phenyl)piperazine 735904, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; PROSIDION LIMITED; WO2007/3964; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution containing 2 7g (18 9 mmol) of 1-[2-(methyloxy)ethyl]piotaperaziotane and 20 mL of THF at O0C was added 0 9 g (23 mmol) of a 60% suspension of sodium hydride in mineral oil The reaction mixture was allowed to stir for 15 mm and 3 O g (18 9 mmol) of 2-chloro-5-niotatropyriotadiotane was added The reaction mixture was heated at 60 0C overnight and then quenched by the addition of H2O and extracted with EtOAc The combined organic layers were dried over MgSO4 and the solvents were removed under reduced pressure The residue was subjected to silica gel chromatography to give 2 7g (54%) of 1-[2-(methyloxy)ethyl]-4-(5-niotatro-2- pyriotadiotanyl)piotaperaziotane as a yellow solid 1 H-NMR (400 MHz, DMSO-cfe) delta 8 95 (d, J = 2 8 Hz, 1 H), 8 21 (dd, J = 9 6 and 2 8 Hz, 1 H), 6 94 (d, J = 9 7 Hz, 2 H), 3 71 – 3 78 (m, 4 H), 3 46 (t, J = 5 7 Hz, 2 H), 3 24 (s, 3 H), and 2 50 – 2 53 (m, 6 H)

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE LLC; ADJABENG, George; BAUM, Erich; BIFULCO, Neil; DAVIS-WARD, Ronda, G.; DICKERSON, Scott, Howard; DONALDSON, Kelly, Horne; HORNBERGER, Keith; PETROV, Kimberly; RHEAULT, Tara, Renae; SAMMOND, Douglas, McCord; SCHAAF, Gregory, M.; STELLWAGEN, John; UEHLING, David, Edward; WATERSON, Alex, Gregory; WO2010/104899; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide A mixture of EXAMPLE 337J (3.0 g), EXAMPLE 337M (1.98 g), N,N-dimethylpyridin-4-amine (1.93 g) and N1-((ethylimino)methylene)-N3,N3-dimethylpropane-1,3-diamine hydrochloride (1.31 g) in dichloromethane (50 ml) was stirred overnight and concentrated. The residue was purified by reverse chromatography, eluted with 40%-70% acetonitrile in 0.1% TFA water. The desired fractions were concentrated to remove acetonitrile, neutralized with NaHCO3 and extracted with dichloromethane. The organic layer was dried over Na2SO4, concentrated and dried to provide the title compound. 1H NMR (400 MHz, dimethylsulfoxide-d6) delta 11.68 (s, 1H), 8.52-8.58 (m, 2H), 8.04 (d, 1H), 7.79 (dd, 1H), 7.53 (d, 1H), 7.47-7.52 (m, 2H), 7.30-7.37 (m, 2H), 7.07 (d, 1H), 7.01-7.06 (m, 2H), 6.68 (dd, 1H), 6.39 (dd, 1H), 6.19 (d, 1H), 4.25 (s, 1H), 3.25-3.32 (m, 4H), 3.07 (s, 4H), 2.75 (s, 2H), 2.09-2.24 (m, 6H), 1.95 (s, 2H), 1.50-1.73 (m, 5H), 1.28-1.43 (m, 4H), 1.06-1.18 (m, 5H), 0.92 (s, 6H)., 1235865-77-6

The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ABBOTT LABORATORIES; US2010/305122; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 : DIPEA (879 mu, 5.17 mmol) was added to 5-bromo-2-chloropyrimidine Ex.10a (500 mg, 2.56 mmol) in acetonitrile (12 mL). Then, benzyl piperazine-1-carboxylate (500 mu, 2.56 mmol) was added to the mixture. The reaction mixture was stirred at r.t. for 60h. Water and EtOAc were added. The two phases were separated and the aqueous solution was extracted with EtOAc. The combined organic layers were dried over MgSO4, filtered and the solution was concentrated to dryness. The crude material was purified by column chromatography on silica gel eluting with Heptane/EtOAc from [100:0] to [0:100]. The product fractions were combined and concentrated to dryness to afford benzyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate Ex.10a (858 mg, 88percent) as white solid.

31166-44-6, The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GENFIT; DELHOMEL, Jean-Francois; PERSPICACE, Enrico; MAJD, Zouher; PARROCHE, Peggy; WALCZAK, Robert; BONNET, Pascal; FOGHA, Jade; (76 pag.)WO2018/138356; (2018); 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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

General procedure: 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., 262368-30-9

The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference：
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