Month: April 2021

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

To a solution of 0.31 mmol 2-isopropylsulfanyl-5-nitro-benzoic acid in 5 ml tetrahydrofuran were added successively 0.31 mmol TBTU, 0.84 mmol N-ethyldiisopropylamine and 0.22 mmol 1-(4-trifluoromethylphenyl)-piperazine (commercially available, e.g. from Fluorochem). The reaction mixture was stirred at 35 C. for 16 h and then concentrated in vacuo. Chromatography (SiO2, ethyl acetate/heptane) followed by trituration in pentane afforded the title compound as a yellow solid (yield 83%). MS (m/e): 454.4 (M+H+, 100%)., 30459-17-7

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

Reference£º
Patent; Jolidon, Synese; Narquizian, Robert; Norcross, Roger David; Pinard, Emmanuel; US2006/149062; (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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

5747-48-8, A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of l l-piperazinyldibenzo[b,fj [l,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25- 30C, to which, was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 mole)] and 2-(2-chloroethoxy) ethanol [32.0 gm ( 0.257 moles)] at room temperature. The reaction mixture was heated to reflux at 110- 112C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check for absence of compound IV) and was cooled to at 25C to 30C,and was added 150 cc DM water, the reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extract and the organic layer were combined, and the pH was adjusted to 2-3 using IN HCl solution in DM water, the reaction mixture was stirred for 30 min at 25-3O0C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH was adjusted to 8-10 using sodium carbonate, the reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extract with 125 cc toluene. The extract and the organic layer were combined, and washed with DM water 300 cc twice. The organic layer was distilled off under vacuum below 500C leaving 50-60 cc toluene with product. Purity of 2-(2-(4- dibenzo[b,f]-[l,4] thiazepine- l l-yl-l-piperazinyl)ethoxy) ethanol in toluene was 99.0% (area % by HPLC). To this solution 1000 cc absolute ethanol was added with activated carbon 5.0 gm and heated to reflux for 90 min. The resulting solution was cooled to 50-550C and filtered. The resulting solution was added 12.5 gm (0.5 moles) fumaric acid at 500C. The reaction mixture was heated to reflux for 2 hrs and was slowly cooled to room temperature and maintained for 2 hrs at room temperature. The reaction mass was filtered and washed with 200 cc absolute ethanol. The wet material obtained was dried under vacuum at 50-55C to afford quetiapine fumarate. Dry weight of quetiapine fumarate is 60-65 gm. Purity of quetiapine fumarate was 99.5% (area % by HPLC).

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/121415; (2008); A2;,
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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

A mixture of 1,4-dibromobenzene (470 mg, 2.0 mmol), 1 -methylpiperazin-2-one hydrochloride (150mg, 1.0 mmol, from J&W PharmLab), palladium acetate (6.7 mg, 0.030 mmol), (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (0.035 g, 0.060 mmol), and cesium carbonate (0.98 g, 3.0 mmol) in toluene (5.0 mL) was evacuated and refilled with nitrogen three times and then the reaction was stirred at 105C. overnight. The mixture was diluted with ethyl acetate, washed with water, brine, then dried over Na2SO4, filtered and concentrated. The residue was purified by flash chromatography on a silica gel column with ethyl acetate in hexane (0-60%) to afford the desired product (0.26 g, 49%). LCMS calculated for C11H14BrN2O (M+H)+:m/z=269.0. Found 269.0., 109384-27-2

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

Reference£º
Patent; Incyte Corporation; Lu, Liang; He, Chunhong; Yao, Wenqing; US2014/45814; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

278788-66-2, Step E: tert-butyl (3R)-4-[ 5-cyano-2-fluoro-4-methoxyphenyl)-2-oxoethyl]-3 -(hydroxymethyl)piperazine-1-carboxylate: To a 250 mL flask was added 5-(bromoacetyl)-4-fluoro-2-methoxybenzonitrile (2.00 g, 7.35 mmol), (R)-N-Boc-2-hydroxymethyl-piperazine (3.18 g, 14.7mmol), DIEA (2.57 mL, 14.7 mmol) and THF (50 mL) and stirred at rt for 1 h; LC analysis of the reaction mixture indicated completion of the reaction. The solution was treated with EtOAc(100 mL), washed with brine, dried (Na2S04), filtered and concentrated to dryness. The residuewas then purified over silica gel with the solvent systems of 5% MeOH in DCM to furnish thedesired product. LC/MS: [(M+ l)t =408.

278788-66-2 (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820286, apiperazines compound, is more and more widely used in various fields.

Reference£º
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

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, Preparation of l-methyl-4- f2-(4-{4- beta-ftrifluoromethyl) fl,2,41 triazolo f4,3- blpyridazin-6-vHpiperazin-l-yl}phenoxy)ethyllpiperazin-2-one2-(4- {4-[3-(Trifluoromethyl)[ 1 ,2,4]triazolo[4,3-b]pyridazin-6-yl]piperazin- 1 – yl}phenoxy)ethyl methanesulfonate (300 mg, 0.62 mmol), 1 -methylpiperazin-2-one (339 mg, 0.93 mmol), DIPEA (0.644 mL, 3.70 mmol) and sodium iodide (9.24 mg, 0.06 mmol) were suspended in DMA (3 mL) and sealed into a microwave tube. The reaction was heated to 1500C for 1 hour in the microwave reactor and cooled to room temperature. The reaction mixture was absorbed on to silica, evaporated and purified by flash silica chromatography, elution gradient 0 to 5percent MeOH in DCM. Pure fractions were evaporated to dryness to afford a gum, which was further purified by ion exchange chromatography using an SCX column, eluting from the column with 2M ammonia/MeOH. Further purification by flash silica chromatography, elution gradient 0 to 5percent MeOH in DCM gave 1 -methyl-4-[2-(4- {4-[3-(trifluoromethyl)[l ,2,4]triazolo[4,3-b]pyridazin-6-yl]piperazin- 1 – yl}phenoxy)ethyl]piperazin-2-one (44.0 mg, 14.14percent) as a solid.IH NMR (399.9 MHz, CDC13) delta 2.78 (4H, m), 2.89 (3H, s), 3.15 (4H, m), 3.22 (2H, s), 3.28 (2H, t), 3.71 (4H, m), 4.01 (2H, t), 6.80 (2H, d), 6.86 (2H, d), 7.05 (IH, d), 7.89 (IH, d); m/z = 505 [M+H]+.

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BRADBURY, Robert, Hugh; RABOW, Alfred, Arthur; WO2010/131022; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-(piperazin-1-yl)ethanol (1.000 g, 7.68 mmol) was dissolved in DCM (35.1 ml) and pyridine (0.932 ml, 11.52 mmol) followed by DMAP (0.094 g, 0.77 mmol) were added. tert-butylchlorodiphenylsilane (2.368 ml, 9.22 mmol) was added to the solution and the reaction mixture was stirred at room temperature overnight. The reaction mixture was concentrated under reduced pressure and the concentrate was purified by column chromatography (ISCO, eluting with 10% MeOH/DCM) to give the title product (2.73 g, yield: 96%). LCMS: (ESI) m/z 369 [M+H]+.

103-76-4, As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; US2012/35134; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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.

EXAMPLE 20 3-chloro-N-(5-chloro-1H-benzimidazol-2-yl-methyl)4-(4-methyl-3-oxo-piperazin-1-yl-carbonyl)-benzamide Prepared analogously to Example 19c from 2-chloro-4-[N-(5-chloro-benzimidazol-2-yl-methyl)-carbamoyl]-benzoic acid, TBTU, diisopropylethylamine and N-methyl-piperazinone in N,N-dimethylformamide. Yield: 8.7percent

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Boehringer Ingelheim Pharma GmbH & Co. KG; US2004/220169; (2004); 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 a solution of 4 (100 mg, 0.23 mmol) in acetonitrile (CH3CN, 10 mL) was added the corresponding arylpiperazines (1.2 equiv) and potassium carbonate (6.0 equiv). The reaction mixture was stirred at reflux for 16 h. After cooling to ambient temperature, the reaction mixture was filtered through a Buchner funnel. After filtration the filtrate was concentrated in vacuo and the residue was purified by silica gel column chromatography using ethyl acetate/petroleum ether (1:4, v/v) as eluent to afford the corresponding products, and all compounds were recrystallized from trichloromethane and n-hexane.

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Article; Xu, Fang; Chen, Hong; Xu, Jingyi; Liang, Xue; He, Xuelan; Shao, Binhao; Sun, Xianqiang; Li, Bing; Deng, Xiaoliang; Yuan, Mu; Bioorganic and Medicinal Chemistry; vol. 23; 24; (2015); p. 7735 – 7742;,
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.

169447-70-5, Step 1: (S)-tert-butyl 2-methyl-4-(3,4,5-trifluorophenyl)piperazine-1-carboxylate A solution of 5-bromo-1,2,3-trifluorobenzene (1.05 g, 5.0 mmol), (S)-tert-butyl 2-methylpiperazine-1-carboxylate (1.0 g, 5.0 mmol), t-BuONa (720 mg, 7.5 mmol), BINAP (62 mg, 0.1 mmol), and Pd2(dba)3 (92 mg, 0.1 mmol) in dry toluene (20 mL) was stirred for 17 hrs at 80 C. The crude product was purified by chromatography (silica, EtOAc/PE=1/30) to afford (S)-tert-butyl-2-methyl-4-(3,4,5-trifluorophenyl)piperazine-1-carboxylate (0.9 g, 2.7 mmol, 54%) as a yellow oil. ESI-MS (EI+, m/z): 275.0 [M-56]+.

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

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Step B: (3-Hvdroxymethyl-benzorib1thioDhen-5-yl)-(4-isoDroDyl-DiDerazin-1 – vD-methanone; . To a suspension of (5-bromo-benzo[iotab]thiophen-3-yl)-nnethanol (130 mg, 0.53 mmol), 1 -isopropyl-piperazine (205 mg, 1.6 mmol), 1 ,8- diazabicyclo[5.4.0]undec-7-ene (DBU; 244 mg, 1.6 mmol), tBu3PBF4 (15 mg, 0.05 mmol) and trans-di-m-acetatobis[2-(di-o-tolylphosphino)benzyl]di-palladium (II) (Hermann’s catalyst; 25 mg, 0.03 mmol) in THF was added Mo(CO)6 (141 mg, 0.53 mmol) and the reaction mixture was sealed and heated at 125 0C with microwave irradiation for 8 min. The solution was concentrated and the resulting residue was partitioned between EtOAc and 1 N NaOH (25 ml_). The organic layer was washed with brine (250 ml_), dried, and concentrated. The resulting residue was purified by FCC to provide 30 mg (18percent) of the title compound as a colorless oil. MS (ESI): mass calcd. for Ci7H22N2O2S, 318.44; m/z found, 319.2 [M+H]+. 1H NMR (CDCI3): 7.88-7.84 (m, 2H), 7.42 (s, 1 H), 7.39-7.35 (m, 1 H), 4.88 (s, 2H), 3.82 (br s, 2H), 3.46 (br s, 2H), 2.73 (h, J = 6.4, 1 H), 2.51 (br s, 2H), 2.36 (br s, 2H), 1.06 (d, J = 6.4, 6H).

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/109333; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics