Category: piperazines

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Bromo-iV -[4-chloro-3-methoxyphenyl]-iV2-(4-[4-(l,l- dimethylethoxy)carbonylpiperazin-l-yl]phenyl)pyrimidine-2,4-diamine (MA2-010): This was obtained by stirring MA2-004 (0.698 g) and 4-(4-tert-butoxycarbonylpiperazino)aniline (0.555 g) in isopropanol (4 mL) at 85 C (oil bath) for 24 h. The reaction mixture was allowed to cool to room temperature and diluted with water (50 mL) which led to the precipitation of product. The crude product was filtered and washed with water (4 x 10 mL) and hexane (4 x 10 mL) to provide MA2-010 as a grey solid (0.960 g, 81%). Mp: 194-195 C. NMR (400 MHz, DMSO-i acquired at 70 C): delta 8.92 (s, IH, disappeared on D2O shake), 8.41 (s, IH, disappeared on D2O shake), 8.17 (s, IH), 7.43-7.37(m, 3H), 7.34-7.28 (m, 2H), 6.82 (d, J= 9.0 Hz, 2H), 3.75 (s, 3H), 3.50-3.45 (m, 4H), 3.06-3.00 (m, 4H), 1.44 (s, 9H). HPLC-MS (ESI+): m/z 591.2 [100%, (M81Br35Cl+H)+ and (M79Br37 +], 589.2 [70%, (M79B35C1 +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; H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.; SCHOeNBRUNN, Ernst; LAWRENCE, Nicholas, J.; LAWRENCE, Harshani, R.; (257 pag.)WO2016/22460; (2016); A1;,
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70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,70261-82-4

[0172] A suspension of intermediate 31 (50 mg, 0.18 mmol), 4-(4-methyl-piperazin-l- ylmethyl)-phenylamine (50 mg, 0.24 mmol), Pd2(dba)3 (10 mg, 0.011 mmol), Xantphos (13 mg, 0.022 mmol) and cesium carbonate (0.12 g, 0.37 mmol) in dioxane/DMF (3/1, 4 mL) was sealed in a microwave reaction tube and irradiated with microwave at 160 C for 15 min. After cooling to room temperature, the cap was removed and the resulting mixture filtered and the filtered solid washed with DCM. The filtrate was concentrated and the residue purified by flash chromatography on silica gel (DCM to 10% MeOH/DCM)to afford the title compound (35 mg, 44%) as an off white solid.[0173] 1R NMR (500 MHz, DMSOd6): 5 2.11 (s, 3H), 2.15 (s, 3H), 2.20-2.45 (m, 8H), 3.35 (s, 2H), 3.75 (s, 3H), 7.07 (d, J= 8.5 Hz, 2H), 7.28 (d, J= 8.5 Hz, IH), 7.44 (dd, J= 8.7, 2.3 Hz, IH), 7.47 (d, J= 2.3 Hz, IH), 7.57 (d, J= 8.5 Hz, 2H), 7.91 (s, IH), 8.36 (s, IH), 8.98 (s, IH). MS (ES+): m/z 453 (M+H)+.

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TARGEGEN, INC.; WO2007/53452; (2007); A1;,
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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

2 – ((1H-pyrrolo [2,3-b] pyridin-5-yl) oxy) -4- (4 – ((4′-chloro-5,5-dimethyl- (0.191 g, 0.335 mmol, 1 eq) (see Step 14 of Example 1), and the title compound was prepared from 6-tetrahydro- [1,1′-biphenyl]4- (2- (4-oxaspiro [2.4] heptan-6-yloxy) ethoxy) -3-nitrobenzenesulfonamide (0.120 g, 0.335 mmol, 1 eq)EDCI (0.077 g, 0.402 mmol, 1.2 eq), DMAP (0.123 g, 1.00 mmol, 3 eq) and 10 mL DCM were placed in a one-necked flask at 0 C for half an hour and then reacted at room temperature. TLC was complete. Quenching reaction, liquid separation, organic phase drying, spin drying, column chromatography EA: DCM = 1: 1 to get the product 0.150g, yield 49%.

1235865-77-6, As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference£º
Patent; Sunshine Lake Pharma Co.,Ltd.; Kou, Yuhui; Hu, Bolin; Jiang, Haigang; Ye, Jiuyong; Liu, Zhiqiang; Xie, Hongming; Zhang, Yingjun; (42 pag.)CN106565706; (2017); A;,
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122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To Int-17 (50 mg, 0.148 mmol) and 2-methoxy-4- (4-methylpiperazin-l-yl) aniline (33 mg, 0.148 mmol) in MeOH (1 mL), 2 drops of 4 M HC1 (aq.) was added. The solution was irradiated under microwave conditions for 30 minutes at 160 C. The solution was transferred to a separatory funnel with EtOAc (40 mL), and washed with saturated NaHCCb (10 mL). The aqueous layer was re-extracted with EtOAc (2 x 20 mL). The organic layers were combined, dried (Na2S04), filtered, and concentrated under reduced pressure. The resulting crude mixture was purified by flash chromatography (S1O2) eluting with DCM in MeOH (0% to 10%) to provide the title compound as a thin film (27 mg, 35%). HPLC: 94% [tR = 5.9 min, 45% MeOH, 55% water (with 0.1% TFA), 20 min]. NMR (400 MHz, DMSO-d6): delta 7.87 (d, / = 8.8 Hz, 1H), 7.85 (s, 1H), 7.40 (d, / = 8.1 Hz, 2H), 7.31 (t, / = 6.8 Hz, 1H), 7.29 (s, 1H, disappeared on D20 shake), 7.23 (t, / = 8.1 Hz, 1H), 6.60 (d, / = 2.5 Hz, 1H), 6.43 (dd, / = 8.8, 2.5 Hz, 1H), 3.82 (s, 3H), 3.59 (q, / = 6.8 Hz, 2H), 3.18 (d, / = 6.8 Hz, 3H from methanol), 3.10-3.04 (m, 4H), 2.46-2.41 (m, 4H), 2.20 (s, 3H). HPLC-MS (ESI+): m/z 523.2 [25%, (M35C135C137C1+H)+], 521.2 [25%, (M35C135C135C1+H)+], 262.2 [100%, (M35C135C137C1+2H)2+], 261.2 [95%, (M35C135C135C1+2H) 2+]. LC-MS (ESI+): 521.2 [100%, (M35C135C135C1+H)+]. HRMS (ESI+): m/z calcd for C24H27Cl3N60 (M+H)+ 521.1385, found 521.1390.

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference£º
Patent; H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE; MAHAJAN, Nupam P.; MAHAJAN, Kiran N.; LAWRENCE, Nicholas J.; LAWRENCE, Hirshani R.; (85 pag.)WO2017/23899; (2017); 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.474711-89-2,Piperazine-1-carboxamide hydrochloride,as a common compound, the synthetic route is as follows.,474711-89-2

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (300mg, 0.64mmol), piperazine-1-carboxamidecompound hydrochloride (127mg, 0.77mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbon Carbodiimidehydrochloride (250mg, 1.3mmol) and N- hydroxy-7-aza-benzotriazole (130mg, 0.96mmol) was dissolved indichloromethane (15 mL), at 0 C conditions, to this solution was added dropwise N, Ndiisopropylethylamine(0.44mL, 2.56mmol), stirred at room temperature 5H, water (10mL ¡Á 3) washing theorganic phase was dried over anhydrous Na 2 SO 4, the solvent was removed concentrate was subjected tocolumn chromatography (eluent: DCM / MeOH (V / v) = 40/1), to give 250mg white solid, yield: 70%.

As the paragraph descriping shows that 474711-89-2 is playing an increasingly important role.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
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182618-86-6, 1-Boc-4-(4-Nitrophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

ferf-Butyl 4-(4-nitrophenyl)piperazine-1-carboxylate (11) (3.24 g, 10.5 mmol) was dissolved in EtOAc (90 mL) under an atmosphere of nitrogen and a slurry of 10% Pd/C (0.500 g) in EtOAc (10 mL) was added. The resulting suspension was then stirred vigorously under an atmosphere of hydrogen at room temperature for 42 hours. The catalyst was removed by filtration through Celite, which was washed with EtOAc (7 x 10 mL) and the solvent was removed in vacuo to give the title compound (12) (2.92 g, 99 % yield) as a pale pink solid; 1H NMR (400 MHz, oVDMSO) delta 6.72 – 6.66 (m, 2H), 6.52 – 6.45 (m, 2H), 4.60 (s, 2H), 3.44 – 3.39 (m, 4H), 2.87 – 2.79 (m, 4H), 1.41 (s, 9H). LCMS Method C: rt 4.40 min; m/z 278.2 [M+H]+., 182618-86-6

As the paragraph descriping shows that 182618-86-6 is playing an increasingly important role.

Reference£º
Patent; CANCER THERAPEUTICS CRC PTY LIMITED; HOLMES, Ian, Peter; BERGMAN, Ylva; LUNNISS, Gillian Elizabeth; NIKAC, Marica; CHOI, Neil; HEMLEY, Catherine Fae; WALKER, Scott Raymond; FOITZIK, Richard Charles; GANAME, Danny; LESSENE, Romina; WO2012/110773; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics

53788-49-1, tert-Butyl 4-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,53788-49-1

Indole-2-carboxylic acid (5.2 g) in THF (200 mL) was treated with carbonyldiimidazole (4.8 g) and stirred at ambient temperature for 10 min whereupon 4-methyl-piperazine-1-carboxylic acid tert-butyl ester (5.0 g) was added. The mixture was stirred at ambient temperature for 72 h and the solvent removed under reduced pressure. The residue was dissolved in ethyl acetate and washed with saturated sodium bicarbonate solution. The organic portion was separated, dried over sodium sulfate and filtered, and solvent was evaporated to afford a solid. Recrystallization from hot ethanol afforded 4-(1 H-Indole-2-carbonyl)-piperazine-1-carboxylic acid tert-butyl ester (4.2 g).

The synthetic route of 53788-49-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Janssen Pharmaceuticals, Inc.; CARRUTHERS, Nicholas, I.; CHAI, Wenying; DVORAK, Curt, A.; EDWARDS, James, P.; GRICE, Cheryl, A.; JABLONOWSKI, Jill, A.; KARLSSON, Lars; KHATUYA, Haripada; KREISBERG, Jennifer, D.; KWOK, Annette, K.; LOVENBERG, Timothy, W.; LY, Kiev, S.; PIO, Barbara; SHAH, Chandravadan, R.; SUN, Siquan; THURMOND, Robin, L.; WEI, Jianmei; XIAO, Wei; (87 pag.)EP1373204; (2016); B1;,
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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

A mixture of 1 -bromo-4-iodobenzene (0.87 g, 3.1 mmol), 4-methylpiperazin-2- one (0.30 g, 2.6 mmol), 3P04 (1.1 g, 5.1 mmol), trans-N, N’-dimethylcyclohexane-l ,2-diamine (0.08 mL, 0.51 mmol) and dioxane (5 mL) was purged with argon gas for 10 min. Copper(I) iodide (0.049 g, 0.26 mmol) was added, the vial sealed and heated at 110 C in an oil bath for 22 h. The reaction was then allowed to cool to rt and was diluted with EtOAc and saturatedNaHC03 was added. The resulting mixture was extracted with EtOAc and the combined organic extracts were dried over MgS04 and concentrated to give the crude product. Purification by silica gel chromatography (MeOH/CH2Cl2, 5:95 to 1 :9) gave an inseparable 2: 1 mixture of the desired product and l-(4-bromophenyl)-4-methylpiperazin-2-one (200 mg). NMR (400 MHz, CDCI3) 6 7.66 (d, J = 8.0 Hz, 2H), 7.02 (d, J = 8.0 Hz, 2H), 3.64 (t, J = 5.0 Hz, 2H), 3.22 (s, 2H), 2.73 (t, J = 5.0 Hz, 2H), 2.35 (s, 3H); MS ESI 317.1 [M + H]+, calcd for [C, ,H|3IN20+ H]+ 317.01.

34770-60-0, As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference£º
Patent; UNIVERSITY HEALTH NETWORK; PAULS, Heinz, W.; LI, Sze-Wan; SAMPSON, Peter Brent; FORREST, Bryan T.; WO2012/48411; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics

70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,70261-82-4

To a solution of 4-(3-(4-cyanophenyl)imidazo[1,2-a]pyridin-6-yl)benzoic acid (70 mg, 0.206 mmol) in DMF (1.0 mL) were added HATU (117 mg, 0.309 mmol), N-methyl morpholine (90 muL, 0.824 mmol) and 4-((4-methylpiperazin-1-yl)methyl)aniline (51 mg, 0.309 mmol). The reaction mixture was stirred at room temperature under inert atmosphere for 18 h, then it was diluted with water (15 mL) and extracted with EtOAc (3*30 mL). The combined organic layer was dried over Na2SO4 and was concentrated under reduced pressure. The residue was purified by preparative HPLC (C18, eluent ACN, water, formic acid 0.1%) to afford 4-(3-(4-cyanophenyl)imidazo[1,2-a]pyridin-6-yl)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)benzamide (40 mg, 37%, AUC HPLC 99%) as a white solid. 1H NMR (400 MHz, CD3OD) delta 8.78 (s, 1H), 8.05 (d, J=8.4 Hz, 2H), 7.96-7.90 (m, 4H), 7.84 (s, 1H), 7.83 (d, 0.1=8.4 Hz, 2H), 7.80-7.76 (m, 2H), 7.68 (d, J=8.8 Hz, 2H), 7.34 (d, J=8.4 Hz, 2H), 3.56 (s, 2H), 2.70-2.40 (m, 8H), 2.36 (s, 3H); 13C NMR (100 MHz, CD3OD): delta 168.12, 147.47, 141.62, 139.17, 135.76, 134.82, 134.74, 134.53, 134.40, 131.08, 129.56, 129.44, 128.49, 128.30, 127.79, 126.61, 122.95, 122.18, 119.51, 118.48, 112.72, 63.14, 55.55, 53.15, 45.65; MS (ESI) m/z 527 [C33H30N6O+H]+.

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Agency for Science, Technology and Research; Nacro, Kassoum; Duraiswamy, Athisayamani Jeyaraj; Rao, Lohitha; US2014/371199; (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.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,as a common compound, the synthetic route is as follows.

2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl)methyl)piperazin-1-yl)benzoic acid (100 mg, 0.175 mmol)Ethyl 8-(2-nitro-4-aminosulfonylphenylamino)octanoate 68mg (0.175mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride (EDCI) 167mg (0.875mmol), 4- dimethylaminopyridine 25.6mg (0.21mmol) ,With anhydrous DCM as solvent, at room temperature for 24h. After the reaction was completed, with 1 M hydrochloric acid,Saturated sodium bicarbonate, saturated brine, the aqueous phase was extracted with EA, the organic phase was combined,Concentration gave 160 mg of a solid which was purified by column chromatography with a yield of 85%., 1235865-77-6

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

Reference£º
Patent; Second Military Medical University; Zheng Canhui; Zhu Ju; Zhou Youjun; Wang Zhongqing; Wang Mingping; Yang Chao; Tian Wei; (18 pag.)CN106957315; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics