Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 109a (R)-tert-Butyl 3-Methyl-4-(6-nitropyridin-3-yl)piperazine-1-carboxylate 109a A 100-mL single-neck round-bottomed flask equipped with a magnetic stirrer and reflux condenser was charged with 1,4-dioxane (60 mL), 5-bromo-2-nitropyridine (2.0 g, 10.0 mmol), (R)-tert-butyl 3-methylpiperazine-1-carboxylate (2.0 g, 10.0 mmol), and cesium carbonate (6.5 g, 20 mmol). See . After bubbling nitrogen through the resulting mixture for 30 minutes, XantPhos (579 mg, 1.0 mmol) and tris(di-benzylideneacetone)dipalladium(0) (915 mg, 1.0 mmol) were added, and the reaction mixture was heated at 100 C. for 15 h. After this time the reaction was cooled to room temperature and filtered. The filtrate was partitioned between ethyl acetate (100 mL) and water (100 mL). The aqueous layer was separated and extracted with ethyl acetate (150 mL*3). The combined organic layer was washed with brine (50 mL) and dried over sodium sulfate. The drying agent was removed by filtration and the filtrate was concentrated under reduced pressure. The residue was purified on flash column eluting with 30:1 DCM/MeOH to afford 109a (1.6 g, 44%) as a yellow solid. MS: [M+H]+ 323. 1H NMR (500 MHz, DMSO) delta 8.21 (d, J=3.5, 1H), 8.18 (d, J=9.0, 1H), 7.43-7.45 (m, 1H), 4.33 (s, 1H), 3.92-3.99 (m, 1H), 3.80 (d, J=12.5, 2H), 3.06-3.23 (m, 3H), 1.43 (s, 9H), 1.09 (d, J=6.5, 3H).

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GENENTECH, INC.; Crawford, James John; Young, Wendy B.; US2013/116245; (2013); A1;,
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21416-67-1, 4,4′-(Propane-1,2-diyl)bis(piperazine-2,6-dione) is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At the beginning of each working day the capillary was flushed with NaOH 0.1M for 10min, 5min with Milli-Q water and 40min with the buffer in basic conditions and with MeOH for 5min, NaOH 1M for 25min, 5 min with Milli-Q water, 5min with HCl 0.1M and 30min with the buffer in acid conditions. In order to ensure the repeatability between injections, the capillary was flushed with NaOH 0.1M for 5min, 5min with the buffer and 2min with the BGE in basic or acid conditions. Buffer solutions were prepared by dissolving the appropriate amount of formic acid, acetic acid, ammonium bicarbonate or boric acid in Milli-Q water, adjusting the pH to the desired value (pH 2.5, 5.0, 7.0, or 9.0, respectively) with 0.1 or 1M NaOH before completing the volume with water to get the desired buffer concentration. Finally, BGEs were prepared by dissolving the appropriate amount of the chiral selectors in the buffer solution. Stock standard solutions of racemic captopril, econazole and clenbuterol were prepared by dissolving the appropriate amount of these drugs in MeOH and razoxane was prepared by dissolving the appropriate amount in Milli-Q water/25% DMF (v/v). These solutions were stored at 4C. All solutions (buffers and standards) were filtered through 0.45mum pore size nylon membrane filters before their injection in the CE system., 21416-67-1

The synthetic route of 21416-67-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Quintana, Sara; Garcia, Maria Angeles; Marina, Maria Luisa; Gomez, Rafael; de la Mata, F. Javier; Ortega, Paula; Tetrahedron Asymmetry; vol. 28; 12; (2017); p. 1797 – 1802;,
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31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,31166-44-6

Step 1 Preparation of Compound 132To a suspension of NaOt-Bu (3.73 g, 38.9 mmol), Pd(dba)2 (0.298 g, 0.518 mmol), RuPhos (0.484 g, 1.036 mmol) and 2-bromo-l,4-difluorobenzene (5 g, 25.9 mmol) in Toluene (50 ml) was added benzyl piperazine-l-carboxylate (6.00 ml, 31.1 mmol) at r.t. under N2.The mixture was stirred at 100¡ãC under N2 for 1 hr. The reaction mixture was diluted with H20 and AcOEt at r.t., then the resulting solid was filtered, rinsed with AcOEt and H2O.The filtrate was extracted with AcOEt x 2. The organic layers were combined and washed with brine. The organic layer was dried over MgS04, filt and cone. The crude product was added to a silica gel column and was eluted with AcOEt-Hexane. Collected fractions were evaporated. The residual oil was triturated with CH2C12-Hexane, then filtered, rinsed with Hexane to afford compound 132 (3.7 g, 43.0 percent) as a white solid.1H-NMR (CDC13) delta: 7.40-7.29 (5H, m), 7.01-6.89 (1H, m), 6.66-6.56 (2H, m), 5.16 (2H, s), 3.67 (4H, t, J= 5.1 Hz), 3.11-2.97 (4H, m).

As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Patent; Shionogi & Co., Ltd.; KUROSE, Noriyuki; WO2011/162409; (2011); A1;,
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Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

INTERMEDIATE 5 (S)-(4-Methyl-piperazin-2-yl)-methanolTo a stirred suspension of (S)-piperazine-l,3-dicarboxylic acid l-tert-buty ester (5.00 g, 21.7 mmol) in THF (40 mL) was slowly added 1.0 M borane-THF complex solution (32.6 rnL, 32.6 mmol). The reaction was heated to 90 0C and stirred under reflux for 2 hours. The reaction mixture was removed from the heat before a further 1.5 equivalents of 1.0 M borane-THF complex solution (32.6 mL, 32.6 mmol) was added. The reaction was reheated to 90 0C and stirred under reflux for a further 2 hours. The reaction was cooled to 0 0C and quenched by the slow addition of MeOH. The reaction mixture was then concentrated in vacuo. The white solid obtained was dissolved in THF (30 mL), cooled to 0 0C and slowly added a 2.0M solution of LiAlH4 in THF (27 mL, 54.0 mmol). The reaction was heated to 90 0C and stirred under reflux for 2h. A further portion of 2.0M solution of LiAlH4 in THF (27 mL, 54.0mmol) was added and the reaction stirred under reflux for 4h and then at room temperature overnight. The reaction mixture was cooled to O0C and quenched by the slow addition of 1.0M aq NaOH solution until the exothermic reaction subsided. The resulting gel was diluted with THF and the solids filtered off. The filtrate was then concentrated in vacuo to afford (S)-(4-methyl-piperazin-2-yl)-methanol (2.84 g, 101% crude yield) as a colourless oil., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOVITRUM AB (PUBL); WO2009/71658; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-fluoro-4- (N-t-butoxycarbonylpiperazin-1-yl) aniline (16.8 g, 57 mmol) (obtained according to the procedure described in preparation 3) in THF (30 ml), dimethyl aniline (7.92 ml, 62. 7 mmol) was added. To this benzyl chloroformate (8.27 ml, 58. 14 mmol) dissolved in THF (20 ml) was added over a period of 20 min upon stirring at 0 C. After completion of the reaction, the resulting mixture was quenched with saturated NaCl solution (50 ml) and extracted with EtOAc (3 x 200 ml). The organic layer was evaporated, dried over Na2S04 and purified using silica gel column using 50% EtOAc in hexane to afford the title compound (24 g).

154590-35-9, 154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Orchid Chemicals &amp Pharmaceuticals Ltd; WO2004/18439; (2004); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A 100 mL round-bottom flask was charged with 2-chloro-4-(morpholin-4- yl)benzaldehyde (0.800 g, 3.54 mmol, 1.00 equiv), tert-butyl (2S)-2-methylpiperazine-l- carboxylate (0.783 g, 3.91 mmol, 1.10 equiv) , 1,2-dichloroethane (20 mL). The mixture was stirred for 30 min at room temperature. Sodium triacetoxyborohydride (2.26 g, 10.7 mmol, 3.00 equiv) was added. The resulting solution was stirred overnight at room temperature, diluted with ]0 (30 mL), extracted with dichloromethane (3 x 30 mL) and the organic layers were combined, dried over Na2S04, filtered and concentrated under reduced pressure. The residue was chromatographed on a silia gel column with ethyl acetate/petroleum ether (25/75) to provide 1.20 g (74% yield) of tert-butyl (2S)-4-[[2-chloro-4-(morpholin-4- yl)phenyl]methyl]-2-methylpiperazine-l-carboxylate as a white solid. LCMS (ESI, m/z): 410 [M+H]+., 169447-70-5

Big data shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; ABIDE THERAPEUTICS; THE SCRIPPS RESEARCH INSTITUTE; CISAR, Justin, S.; GRICE, Chery, A.; JONES, Todd, K.; NIPHAKIS, Micah, J.; CHANG, Jae, Won; LUM, Kenneth, M.; CRAVATT, Benjamin, F.; WO2013/103973; (2013); 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.

Intermediate 46: 1,1-dimethylethyl (3S)-3-(hydroxymethyl)-4-(trifluoroacetyl)-1-piperazinecarboxylate 1,1-dimethylethyl (3S)-3-(hydroxymethyl)-1-piperazinecarboxylate (Commercial) (350 mg, 1.618 mmol) was dissolved in Dichloromethane (DCM) (10 ml) and cooled in an ice bath under nitrogen. Triethylamine (0.564 ml, 4.05 mmol) was added followed by the careful addition of trifluoroacetic anhydride (0.571 ml, 4.05 mmol). After ?10 mins, the ice bath was removed and the reaction was allowed to warm to room temperature and stirred for 3 hours. The reaction was washed with water. The aqueous was extracted with DCM. The combined organics were washed with water, dried using a hydrophobic frit and evaporated in vacuo to give a pale yellow oil (0.69 g) LCMS (Method B): Rt=0.45 min, MH+=245, 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; Atkinson, Francis Louis; Atkinson, Stephen John; Barker, Michael David; Douault, Clement; Garton, Neil Stuart; Liddle, John; Patel, Vipulkumar Kantibhai; Preston, Alexander G.; Shipley, Tracy Jane; Wilson, David Matthew; Watson, Robert J.; US2014/5188; (2014); 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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a solution of 53 7-bromo-4,6-dichloro-3-nitroquinoline (2.07 g, 6.43 mmol) in 78 THF (50 ml) was added 242 1-(tert-butyl) 3-methyl piperazine-1,3-dicarboxylate (2.356 g, 9.64 mmol) followed by 56 DIPEA (3.36 ml, 19.29 mmol) under nitrogen. The reaction was then heated at reflux overnight, cooled and evaporated, taken up in water and extracted with DCM then dried by passing through a phase separator cartridge. Evaporation afforded an orange gum which was purified by flash silica chromatography, elution gradient 0 to 50% 57 EtOAc in 58 heptane. Pure fractions were evaporated to dryness to afford 243 1-(tert-butyl) 3-methyl-4-(7-bromo-6-chloro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (1.66 g, 49%) as a yellow foam. 1H NMR (400 MHz, DMSO, 30 C.) 1.45 (9H, s), 3.30 (1H, s), 3.55 (3H, s), 3.59-3.69 (1H, m), 3.72 (1H, d), 3.75 (1H, d), 3.84 (1H, s), 4.11 (1H, s), 4.35 (1H, s), 8.50 (1H, s), 8.54 (1H, s), 9.12 (1H, s). m/z: ES+ [M+H]+ 529., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); 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.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

A solution of 4-(2,4-dichloro-phenyl)-1H-pyrazole-3-carboxylic acid (70 mg; 0.27 mmol), 4-(4-methyl-piperazin- 1-yl)-benzylamine (62 mg; 0.3 mmol), EDAC (63 mg; 0.33 mmol) and HOBt (45 mg; 0.33 mmol) in 5 ml of DMF was stirred at room temperature for 48 hours. The reaction was evaporated and the residue partitioned between ethyl acetate and brine. The ethyl acetate layer was separated, dried (MgSO4), filtered, evaporated then dried further under vacuum to give 34 mg of 4-(2,4-dichloro-phenyl)-1H-pyrazole-3-carboxylic acid 4-(4- methyl-piperazin-1-yl)-benzylamide. (LC/MS: Rt 2.42 [M+H]+444).

216144-45-5, The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; WO2006/77424; (2006); A1;; ; Patent; ASTEX THERAPEUTICS LIMITED; WO2006/77428; (2006); 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.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of 214 mg (1 mmol) tert-butyl (2S,5R)-2,5-dimethylpiperazine-1 – carboxylatein 3.3ml THF were added at RT 1.74 mL DIPEA (10 mmol, 10 eq) and 176 mg benzenesulfonyl chloride (1 mmol, 1 eq) and the mixture was stirred for 3 days at RT. The mixture was evaporated to yield 440 mg (124%) of the crude title compound which was used in the next step without further purification. LC-MS (Method 1 ): Rt = 1 .30 min; MS (ESIpos): m/z = 355 [M+H]+ (0524) 1H-NMR (500 MHz, DMSO-d6) delta [ppm]: 0.81 (3H), 0.99 (3H), 1 .37 (9H), 3.08 – 3.19 (3H), 3.51 – 3.67 (3H), 4.00 – 4.34 (2H), 7.62 (2H), 7.69 (1 H), 7.79 (2H).

548762-66-9, The synthetic route of 548762-66-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; KOPPITZ, Marcus; SIEBENEICHER, Holger; STEUBER, Holger; TER LAAK, Antonius; NUBBEMEYER, Reinhard; ROTTMANN, Antje; IRLBACHER, Horst; BADER, Benjamin; PETERS, Michaele; WAGENFELD, Andrea; (157 pag.)WO2018/114670; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics