Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

Azelaic acid (326 mg, 1.74 mmol), HOBt (1 17 mg, 0.87 mmol), TBTU (279 mg, 0.87 mmol), anhydrous triethylamine (121 ??, 1 .39 mmol) and dry DMF (2 ml) were placed in an oven-dried Schlenk tube under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. A second Schlenk tube was prepared containing 1-(4-trifluoromethyl phenyl) piperazine (200 mg, 0.87 mmol) and dry DMF (1 ml) under a nitrogen atmosphere. The resulting solution was stirred until complete dissolution of the piperazine had occurred. The piperazine solution was then transferred, via a cannula, to the first Schlenk tube containing the carboxylic acid. The resulting solution was stirred for 24 hrs, under nitrogen, and monitored by TLC. After 24 hrs, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M hydrochloric acid solution. The aqueous mixture was extracted with dichloromethane (20 ml, followed by 4 x 10 ml) and the organic layer washed with a saturated sodium bicarbonate solution (3 x 20 ml) and brine (3 x 20 ml). The organic layer was dried over magnesium sulphate and evaporated under reduced pressure. The residue was purified using flash chromatography (DCM followed by 9.5: 0.5, DCM:MeOH) to obtain the desired product as a white solid in a 60% yield. H NMR (300 MHz, CDCI3) ? 7.49 (d, 2H), 6.91 (d, 2H), 3.77-3.78 (m, 2H), 3.62-3.64 (m, 2H), 3.24-3.31 (m, 2H), 2.33- 2.39 (m, 2H), 1.60-1.68 (m, 4H), 1.33-1.38 (m, 6H). MS (+ESI) calcd for C20 H27 F3 N2 03 m/z: [M + H]+, 401 .2047; found 401.2047 [Diff(ppm) = 0].

30459-17-7, 30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH; STEPHENS, John; FINDLAY, John; KINSELLA, Gemma; MARTIN, Darren; DEVINE, Robert; VELASCO-TORRIJOS, Trinidad; WO2013/60860; (2013); A1;,
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13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure P. l-[4-(4-Nitro-phenyl)-piperazin-l-yl]-ethanoneA focus microwave vessel was charged with 4-fluoronitrobenzene (leqv, 1.41 g, 10 mmol), acetylpiperazine (leqv, 1.28 g, 10 mmol), DIPEA (leqv, 1.7 ml, 10 mmol) and propan-2-ol (2 ml). The reaction mixture was irradiated (100W) at 9O0C for 25 mins. A yellow precipitate formed on cooling, which was collected by filtration, washed with propan-2-ol (20 ml) and dried under vacuum to give the product (1.401 g, 56%, 5.6 mmol) as a yellow solid. LC/MS: 100% MH+, m/z 250, Rt = 1.23 mins.

13889-98-0, 13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; EVOTEC AG; WO2008/122787; (2008); A1;,
Piperazine – Wikipedia
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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, To a stirred solution of (2S)-2-methylpiperazine (0.30 g, 2.1 mmol) in DMA (6 mL), 6-chloropyridine-3-carbonitrile (0.29 g, 2.3 mmol) and K2C03 were added. The resultantreaction mixture was heated to 60 C for 2 h (TLC indicated complete consumption ofstarting material). The reaction mixture was diluted with cold water (20 mL) and extractedwith EtOAc (3 x 25 mL). The combined organic extracts were washed with cold water (20mL) and brine (2 x 20 mL). The organic layer was separated, dried over Na2S04 andconcentrated under reduced pressure to give the crude residue which was purified by columnchromatography (100-200 silica gel, 10 g, 10% MeOH-DCM) to furnish 6-[(3S)-3-methylpiperazin-1-yl]pyridine-3-carbonitrile (0.29 g, 67%) as an off-white solid.LCMS: m/z: 203.4 [M+Ht.

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference£º
Patent; MITOBRIDGE, INC.; TAKAHASHI, Taisuke; KLUGE, Arthur; LAGU, Bharat; JI, Nan; (162 pag.)WO2018/125961; (2018); A1;,
Piperazine – Wikipedia
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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.

Example 166 N1-{[1,6-Diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-N1-[(6-methyl-3′-{[(3S)-3-methyl-1-piperazinyl]methyl}-3-biphenylyl)methyl]-1,1-cyclopropanedicarboxamide A mixture of N1-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-N1-[(3′-formyl-6-methyl-3-biphenylyl)methyl]-1,1-cyclopropanedicarboxamide (55 mg, 0.088 mmol), (R)-N’-Boc-2-methyl-piperazine (17.69 mg, 0.088 mmol), sodium triacetoxyborohydride (37.4 mg, 0.177 mmol) and acetic acid (6.07 muL, 0.106 mmol) in DCM (2 mL) was stirred at room temperature overnight. The reaction mixture was quenched with saturated NaHCO3 and extracted with DCM twice. The combined organic layers were concentrated under vacuum to give the crude residue. It was re-dissolved in 25% TFA in DCM (2 mL) and stirred at room temperature for 2 h. Solvent was evaporated under a stream of nitrogen and then purified by reverse phase hplc with a Gilson HPLC (acidic conditions: 0.1% TFA in the solvents), eluding with 10 to 60% CH3CN in water at a flow rate of 20 mL/min. The product fractions were combined, washed with saturated NaHCO3 and extracted with ethyl acetate twice. The combined organic layers were washed with brine, dried over sodium sulfate, filtered and then concentrated under vacuum to give N1-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-N1-[(6-methyl-3′-{[(3S)-3-methyl-1-piperazinyl]methyl}-3-biphenylyl)methyl]-1,1-cyclopropanedicarboxamide as a solid (30 mg, 48.1%). LC-MS m/z 707 (M+H)+, 0.74 min (ret time); 1H NMR (400 MHz, DMSO-d6) delta 0.88 (d, J=6.27 Hz, 3H) 1.20 (t, J=7.53 Hz, 3H) 1.29-1.36 (m, 7H) 1.40-1.64 (m, 3H) 1.84-1.92 (m, 3H) 2.17 (s, 3H) 2.60-2.67 (m, 4H) 2.73-2.78 (m, 1H) 2.83 (q, J=7.36 Hz, 2H) 3.46 (s, 2H) 3.52 (td, J=11.36, 2.13 Hz, 2H) 3.80-3.87 (m, 2H) 4.04-4.11 (m, 1H) 4.21-4.44 (m, 6H) 6.74 (d, J=7.78 Hz, 1H) 7.04 (d, J=1.76 Hz, 1H) 7.07-7.11 (m, 1H) 7.14-7.21 (m, 3H) 7.26 (d, J=7.78 Hz, 1H) 7.34-7.38 (m, 1H) 7.99 (s, 1H) 8.43 (t, J=5.77 Hz, 1H) 9.02 (t, J=5.77 Hz, 1H)., 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; Glaxo Group Limited; US2009/203677; (2009); 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.883554-88-9,4-Carbamoyl-piperazine-1-carboxylic acid tert-butyl ester,as a common compound, the synthetic route is as follows.,883554-88-9

To a solution of tert-butyl4-carbamoylpiperazine-1-carboxylate (0.16 g, 0.7 mmol) in DCM (2 mL) was addeda HCl in EtOAc solution (4 M, 2 mL) . The mixture was stirred at rt for 30 min andconcentrated to give the title compound as a white solid (0.16 g, 100) . 1H NMR (600 MHz, CD3OD): delta ppm 3.71-3.73 (m, 4H) , 3.25-3.27 (m, 4H) and MS-ESI: m/z 130.10[M+H-HCl] + .

883554-88-9 4-Carbamoyl-piperazine-1-carboxylic acid tert-butyl ester 17750351, apiperazines compound, is more and more widely used in various fields.

Reference£º
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

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To the stirred solution of 4-oxo-3, 4-dihydroquinazoline-2-carboxylic acid (0.1 g, 0.0005 mol) in N,N-dimethyl formamideDMF, N-phenyl piperzine derivatives (0.0005 mol),or 3-(4-phenylpiperazin-1-yl)propan-1-amine derivatives(9a-g, 0.0005 mol) were added at room temperature, followedby the addition of EDC HCl (0.0006 mol) and HOBt(0.0006 mol) and the mixture was stirred for 1 h. Aftercompletion of the reaction (TLC analysis), small amount ofice cold water (10 mL) was added to the reaction mixtureand then extracted with chloroform (2 ¡Á 10 mL). Thechloroform layer was separated, dried over Na2SO4, andevaporated under vacuum to give corresponding hybrids(10a-g, 11a-g) in good yields., 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Venkatesh, Ramineni; Kasaboina, Suresh; Janardhan, Sridhara; Jain, Nishant; Bantu, Rajashaker; Nagarapu, Lingaiah; Medicinal Chemistry Research; vol. 25; 9; (2016); p. 2070 – 2081;,
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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

Diethylcyanophosphonate (Aldrich, Buchs, Switzerland; 0.50 mL, 3.0 [MMOL)] is added to a stirred mixture of 3-[[4-(3-pyridinyl)-2-pyrimidinyl] amino] -benzoic acid (438 mg, [1.] 5 [MMOL),] 4- [[ (4-METHYL-1-PIPERAZINYL) METHYL]] benzeneamine (308 mg, 1.5 [MMOL)] and triethylamine (840 [.//L,] 3.0 [MMOL)] in 10 mL N,N-dimethylformamide at [10C.] After stirring for 12 hours at [60C,] the mixture is treated with an aqueous solution of sodium hydrogen carbonate and extracted three times with ethyl acetate. The combined extracts are washed with water, and the solvent is evaporated off under reduced pressure to give a residue. The residue is resuspended in water and filtered to afford the crude product which is recrystallised from tetrahydrofuran- ethyl acetate to give N-[3-[[4-(3-Pyridinyl)-2-pyrimidinyl]amino]-N-[(4-methyl-1-piperazinyl)- methyl] benzamide as a crystalline solid, m. p. [220-224C.], 70261-82-4

70261-82-4 4-(4-Methylpiperazin-1-ylmethyl)phenylamine 3153996, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/5281; (2004); A1;,
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1152367-80-0, (S)-1,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of triphosgene (1.04 g, 3.5 mmol) in DCM (20 mL) under nitrogen was added pyridine (2.3 g, 28.0 mmol) drop-wise at 0 C. followed by addition of (S)-1,3-dimethylpiperazine (800 mg, 7.0 mmol) in DCM (30 mL), the reaction mixture was warmed to RT and stirred overnight as monitored by TLC (Rf=0.9, PE: EtOAc=1:1). The mixture was concentrated to give Intermediate 11 (3 g, crude) which was used without purification.

1152367-80-0, The synthetic route of 1152367-80-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; LI, David Yunzhi; WANG, Jiabing; YANG, Zhenfan; ZENG, Qingbei; ZHANG, Xiaolin; US2014/255428; (2014); 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.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of compound 9 (200mg, 0.8mmol), sodium iodine (289mg, 1.93mmol) and substituted amines (1.61mmol) in methanol (30mL) was stirred at 40C for 5h. After the reaction was completed (monitored by TLC), the solution was concentrated under vacuum. Then the crude residue was purified by column chromatography (dichloromethane/methanol), affording pure product 10., 208167-83-3

The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Liang, Yu-Kun; Yue, Zhi-Zhou; Li, Jia-Xin; Tan, Cun; Miao, Ze-Hong; Tan, Wen-Fu; Yang, Chun-Hao; European Journal of Medicinal Chemistry; vol. 84; (2014); p. 505 – 515;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.350684-49-0,tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The adamantane-1-isocyanate (157 mg, 0.88 mmol) was dissolved in 5 mL of anhydrous dichloromethane. A solution of tert-butyl 4- (4-aminobenzoyl) piperazine-1-carboxylate (5) (270 mg) was added dropwise to a solution of 5 mL of anhydrous dichloromethane at 0 C, 0.88 mmol). The reaction was allowed to warm at room temperature and stirred overnight. After about 12 hours, the reaction was stopped, concentrated, and purified by column chromatography (CH2C12: CH30H = 40: 1) to give 320 mg of a white powder solid in 66% yield.

350684-49-0, The synthetic route of 350684-49-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chinese Academy of Sciences, Shanghai Institute of Medicine; LONG, YAQIU; HUANG, SHAOXU; (71 pag.)CN102464631; (2016); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics