Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, To the 500 mL single neck flask was added 8.5 g (36.2 mmol) of crude I-a,FeO (OH) / C catalyst 2.0 g and 95% ethanol 100 mL,Heating reflux,A mixture of 25 mL of hydrazine hydrate and 20 mL of 95% ethanol was slowly added dropwise,TLC detects the disappearance of the starting material (methanol: chloroform = 1:15).The filter cake was washed twice with hot ethanol (30 mL x 2)The solvent was evaporated under reduced pressure to give a white solid,And dried in vacuo to give 6.7 g of (I-b) in a yield of 90.3%.Products without further purification, directly into the next step.

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; China Pharmaceutical University; Lu Shuai; Wang Yue; Zhi Yanle; Yao Chao; Lu Tao; Li Baoquan; Chen Puzhou; Bao Jiyin; (27 pag.)CN107245073; (2017); A;,
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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

N: l,4-bis(tert-butoxycarbonyl)piperazine-2-carboxylic acid 25. To an aqueous solution of Na2C03 (40 g, 380 mmol, in 200 mL of water) at room temperature was added piperazine-2- carboxylic acid dihydro chloride (either an enantiomeric mixture or a specific stereoisomer) (24; 10 g, 50 mmol), followed by di-ieri-butyl dicarbonate (41 g, 183 mmol) in tetrahydrofuran (200 mL). The reaction mixture was stirred at room temperature for 20 hours and then the volatiles were removed under reduced pressure. The resulting mixture was then extracted with diethyl ether (100 mL). The aqueous layer was treated with 3.0 M HC1 until it was slightly acidic (pH = 4) and then extracted with ethyl acetate (150 mL). The organic layer was washed with brine, dried over anhy. Na2SC>4, filtered, and concentrated to afford 16 g of the title compound as a white solid.

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; AGIOS PHARMACEUTICALS, INC.; CAO, Sheldon; POPOVICI-MULLER, Janeta; SALITURO, Francesco G.; SAUNDERS, Jeffrey; TAN, Xuefei; TRAVINS, Jeremy; YAN, Shunqi; YE, Zhixiong; WO2012/171506; (2012); 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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

a N-(tert-Butoxycarbonyl)-1-(2-hydroxyethyl)piperazine To a solution of 1-(2-hydroxyethyl)piperazine (5.20 g, 40 mmol) and triethylamine (6 mL 43 mmol), in 1,4-dioxane (100 mL) was added slowly di-tert-butyl dicarbonate (8.72 g, 40 mmol). The reaction mixture was stirred at room temperature for 2 h. The solvent was removed in vacuo and the residue was purified by flash column chromatography (ethyl acetate to 2% methanol in ethyl acetate) to give the title compound as colorless oil (8.32 g, 90%). 1 H-NMR (300 MHz, CDCl3) delta 1.46 (s, 9H), 2.46 (t, 4H), 2.55 (t, 2H), 2.75 (br s, 1H), 3.44 (t, 4H), and 3.63 (t, 2H)., 103-76-4

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; 3-Dimensional Pharmaceuticals, Inc.; US6034127; (2000); A;,
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109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example of preparation. Preparing form I gatifloxacin for seeding; 10 g (0.0339 moles, 1 equivalent) of 1- cyclopropyl-6, 7-difluoro-1, 4-dihydrc-8-methoxy-4-oXo-3- quinolinecarboxylic acid (CAS no.: 112811-72-0) is placed in a flask, 30 mL of acetonitryl (3 volumes) is added and the solution is heated to a temperature of 76-80 C. Once reflux has been attained, 3.28 g (0.0203 moles, 0.6 equivalents) of hexamethyldisilazane (HMDS) is added using a compensated addition funnel, maintaining the temperature. Once the addition is completed, the reaction is maintained with stirring for 1 hour at a temperature of 76-80 C. Once this period has elapsed, the reaction mixture is cooled to a temperature between 0 and 15 C, and 5.78 g (0.0407 moles, 1.2 equivalents) of boron trifluoride ethyletherate is added, keeping the temperature below 15 C. Once the addition has finished, the temperature is allowed to rise to 15-25 C and :-t is kept under these conditions for approximately 2 hour : :. The pH of the mixture is then adjusted to an approximate value of 9 with triethylamine (approximately 2 mL). To the resulting suspension : s added a solution of 10.19 g (0.1017 moles, 3 equivalents) of 2-methylpiperazine in 28 mL of acetonitryl, keeping the temperature between 15 and 25 C. The resulting amber solution is kept with stirring under these conditions for approximately 3 hours. Once the reaction has beer : completed, the mixture is distilled at low pressure unti : a stirrable paste is obtained. At this point, 50 mL of methanol is added, the resulting suspension is raised to a temperature of 63-67 C and kept under these conditions for approximately 5 hours. Once the reaction has been completed the mixture is cooled to a temperature of 25-35 C over a water bath and then to a temperature of 0-5 C over a water/ice bath for a further 1 hour. The resulting precipitate is filtered, washed with cold methanol (2 x 10 mL) and dried at 40 C in an oven in vacuo to constant weight. 10.70 g of crude gatifloxacin is obtained, with a water content of 2. 95% by weight. The yield of the process is 81.8%. The crude product obtained is used for the seeding in Example 1. The crude product is crystallised in methanol by dissolving-20 g of crude gatifloxacin in 1 1 of methanol (50 volumes) at a temperature of D3-67 C. Once all the product has been dissolved it is placed to cool to a temperature of 30-40 C, and then to a temperature of 0-5 C over a water/ice bath, maintaining it under these conditions for 1 hour. The resulting suspension is filtered and the solid retained is washed with 20 mL (1 volume) of cold methanol. The solid obtained is dried at 40 C in a vacuum oven to obtain 18.65 g of gatifloxacin with a water content of 2. 36% by weight.

109-07-9, As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; QUIMICA SINTETICA, S.A.; WO2005/47262; (2005); A1;,
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109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-[(S)-1 -(6-chloro-imidazo[1 ,2-b]pyridazin-3-yl)-ethyl]-5,7-difluoro-quinoline (Intermediate B, 3.0 g, 8.58 mmol), KF (2.52 g, 42.9 mmol), 1-methylpiperazine-2-one hydrochloride (3.88 g, 25.7 mmol), N-ethyldiisopropylamine (5.99 ml_, 35 mmol) were suspended in NMP (60 mL). The RM was stirred at 180 0C for 8.5 h. The mixture was diluted with EtOAc and washed with 1M Na2CO3 (1 x) and water (2 x). The aqueous was further extracted with EtOAc (2 x). The combined organic layers were dried over Na2SO4, filtered and concentrated. The residue was purified by flash chromatography and then crystallized in EtOAc to afford the title compound as a white solid (tR 3.19 min (conditions 1), (tR 8.84 min (conditions 2), MH+ = 423.2, 1H-NMR in DMSO-d6: 8.94 (d, 1H); 8.45 (d, 1 H); 7.84 (d, 1 H); 7.63 (s, 1H); 7.59 (m, 2H); 7.08 (d, 1H); 4.98 (m, 1H); 4.02 (d, 1 H); 3.73 (d, 1H); 3.60 (m, 2H); 3.31 (m, 1H); 3.25 (m, 1H); 2.80 (s, 3H); 1.88 (d, 3H))., 109384-27-2

As the paragraph descriping shows that 109384-27-2 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; FURET, Pascal; McCARTHY, Clive; SCHOEPFER, Joseph; STUTZ, Stefan; WO2011/15652; (2011); A1;,
Piperazine – Wikipedia
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59702-07-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

To a solution of 4-(3-(4-cyanophenyl)imidazo[l,2-a]pyridin-6-yl)benzoic acid (70 mg, 0.206 mmol) in DMF (1.0 mL) were added HATU (1 17 mg, 0.309 mmol), N-methyl morpholine (90 iL, 0.824 mmol) and l-methylpiperazin-2-one (37 mg, 0.247 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 Na2S04 and concentrated under reduced pressure. The residue was purified by column chromatography (silica gel, eluent CHCl3 MeOH 96:4) to afford 4-(6-(4-(4-methyl-3- oxopiperazine-l-carbonyl)phenyl)imidazo[l,2-a]pyridin-3-yl)benzonitrile (64 mg, 57percent, AUC HPLC 98percent) as a white solid. 1H NMR (400 MHz, CD3OD) delta 8.76 (bs, 1H), 7.97-7.89 (m, 4H), 7.88 (s, 1H), 7.84-7.78 (m, 2H), 7.77 (d, J= 1.2 Hz, 2H), 7.64-7.57 (m, 2H), 4.40- 4.10 (m, 2H), 4.10-3.60 (m, 2H), 3.57-3.42 (m, 2H), 3.01 (s, 3H); 13C NMR (100 MHz, CD3OD): delta 171.72, 147.44, 140.53, 135.51, 134.81 , 134.72, 134.38, 129.42, 129.27, 128.56, 128.52, 127.79, 126.58, 122.93, 119.50, 1 18.47, 112.70, 34.68; MS (ESI) m/z 436 [C26H21N502 + H] +.

The synthetic route of 59702-07-7 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; CHENNAMANENI, Lohitha, Rao; WO2013/147711; (2013); A1;,
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75336-86-6,75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(6-Chloro-4,5-dimethyl-pyridazin-3-yl)-pyridin-3-yl-methanone (1.2 g, 4.84 mmol) and (R)-2-methyl-piperazine (485 mg, 4.84 mmol) are added to a microwave vial followed by NMP (17 mL) and triethylamine (2.01 mL, 14.49 mmol). The vial is sealed and irradiated in the microwave at 170¡ã C. for 30 min. The crude material is directly purified via flash chromatography on silica gel (0-20percent methanol in CH2Cl2). The resulting oil is co-evaporated with CH2Cl2 and heptane to afford the title compound as a powder (1350 mg, 90percent). 1H NMR (400 MHz, DMSO-d6) delta=9.56 (br s, 1H), 8.96 (s, 1H), 8.84-8.86 (m, 1H), 8.21-8.24 (m, 1H), 7.60-7.63 (m, 1H), 3.72 (s, 1H), 3.69 (s, 1H), 3.45-3.50 (m, 1H), 3.26-3.31 (m, 4H), 2.30 (s, 6H), 1.32 (d, J=6.5 Hz, 3H).

As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference£º
Patent; Novartis AG; US2010/41663; (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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,74879-18-8

EXAMPLE 213A (3S)-3-methyl-1-(2-pyridinyl)piperazine A solution of (S)-(+)-2-methylpiperazine (0.50 g, 0.005 mol, CAS 74879-18-8, Aldrich 39,717-2, 99%) and 2-bromopyridine (5 mL, 0.05 mol) was heated to 120 C. for 14 hours. The reaction mixture was cooled to 23 C. and partitioned between ethyl acetate and water. The layers were separated, and the water layer extracted twice more with ethyl acetate. The aqueous phase was adjusted to pH~11 with a solution of saturated sodium bicarbonate and solid sodium carbonate. Sodium chloride was added, and the saturated aqueous solution was extracted with ethyl acetate (2*) and dichloromethane (2*). The combined organic extracts were dried over sodium sulfate, filtered, and concentrated under reduced pressure to afford 0.6 g (67% yield) of the title compound. 1H NMR (400 MHz, DMSO-d6) delta1.02 (d, J=6.0 Hz, 3H), 2.27 (dd, J=12, 10 Hz, 1H), 2.67 (m, 3H), 2.92 (m, 1H), 4.07 (m, 2H), 6.58 (dd, J=8, 6 Hz, 1H), 6.77 (d, J=8 Hz, 1H), 7.49 (m, 1H), 8.08 (m, 1H); MS (ESI) m/e 178 (M+H)+.

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

Reference£º
Patent; Bhatia, Pramila A.; Daanen, Jerome F.; Hakeem, Ahmed A.; Kolasa, Teodozyj; Matulenko, Mark A.; Mortell, Kathleen H.; Patel, Meena V.; Stewart, Andrew O.; Wang, Xueqing; Xia, Zhiren; Zhang, Henry Q.; US2004/29887; (2004); A1;,
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169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Methyl chloroformate (230 1iL, 3 mmol) was slowly added at 0C to a solution of tert-butyl (25)-2-methylpiperazine-i-carboxylate (300 mg, 1.5 mmol) and triethylamine (835 1iL, 6 mmol) in methylene chloride (6 mL). After stirring at r.t. for 1 h, reaction mixture wascarefully quenched by addition of water and the desired product was extracted with ethyl acetate. The organic phase was washed with brine, dried over sodium sulfate and solvent was evaporated under reduced pressure. Cmde material was purified by Biotage IsoleraTM to give (5)-i -tert-butyl 4-methyl 2-methylpiperazine- 1 ,4-dicarboxylate (378 mg, 97%). LCMS calculated for C7H15N202 (M+H-Boc) m/z = 159.1; found: 159.1., 169447-70-5

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; INCYTE CORPORATION; VECHORKIN, Oleg; LI, Yun-Long; SOKOLSKY, Alexander; WANG, Anlai; ZHU, Wenyu; ZHUO, Jincong; (185 pag.)WO2017/59251; (2017); 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.

To a solution of sodium bicarbonate (6.5 mmol) in water (2 mL) and DCM (10 mL) at 00C is added bromoacetyl bromide (6.5 mmol), followed by immediate addition of 1-cyclopentylpiperazine (3.25 mmol). The mixture is stirred at 00C for an additional 40 min. To the mixture is added aqueous sodium bicarbonate (15 mL) and DCM (30 mL). The layers are separated and the organic layers dried (MgSO^ and solvent removed in vacuo to give the title compound, which is used in the next step reaction without further purification.

21043-40-3, The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NEUROGEN CORPORATION; WO2007/16496; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics