Month: May 2021

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of methyl 1-Boc-piperazine-2-carboxylate (0.5 g, 2 mmol) in CH2Cl2 (10 ml) was added PhSO2Cl (0.53 ml,4.1 mmol) and Et3N (0.57 ml, 4.1 mmol) at room temperature. The resulting solution was stirred overnight. The reaction was washed with 1 N NaHCO3 (40mL x 3), brine and dried over Na2SO4. The product was purified via flash chromatography (10% EtOAc/Hexanes; 20% EtOAc/Hexanes; 50% EtOAc/Hexanes) to give an off-white solid Methyl 1-Boc-4-benzenesulfonyl-piperazine-2-carboxylate in 91% yield., 129799-15-1

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Zhao, Huanyu; Prosser, Anthony R.; Liotta, Dennis C.; Wilson, Lawrence J.; Bioorganic and Medicinal Chemistry Letters; vol. 25; 21; (2015); p. 4950 – 4955;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

52385-79-2, 2-(3-Chlorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 300 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-[3-(2-piperazinyl)phenyl]-1H-indole-7-carboxamide trifluoroacetate To a solution of 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole-7-carboxamide (60 mg, 0.13 mmol) in dioxane (1.5 mL) and water (0.5 mL) was added 2-(3-chlorophenyl)piperazine (63.7 mg, 0.325 mmol) and potassium carbonate (90 mg, 0.650 mmol). This mixture was degassed for 5 min then tetrakis(triphenylphosphine)palladium(0) (12 mg, 0.011 mmol) was added. The resulting mixture was reacted in a microwave for 30 min at 160 C. The solid was filtered off and all solvents were evaporated. The resulting solution was re-dissolved in dichloromethane and separator was used to remove water. The mixture was concentrated to give organic solvent and then purified by Gilson Preparatory HPLC to give 21.7 mg of the title compound (27.4%). LC/MS=m/z 496.4 [M+H] Ret. Time: 1.28 min., 52385-79-2

As the paragraph descriping shows that 52385-79-2 is playing an increasingly important role.

Reference：
Patent; Deng, Jianghe; Kerns, Jeffrey K.; Jin, Qi; Lin, Guoliang; Lin, Xichen; Lindenmuth, Michael; Neipp, Christopher; Nie, Hong; Thomas, Sonia M.; Widdowson, Katherine L.; US2009/143372; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-{4-[3-(6-Bromo-quinazolin-4-yl)-5-fluoro-benzoyl]-piperazin-1-yl}-ethanone To a mixture of 3-(6-bromo-quinazolin-4-yl)-5-fluoro-benzoic acid (1.36 g, 3.72 mmol) in CH2Cl2 (15 mL) was added DIPEA (1.30 mL, 7.44 mmol) and HBTU (1.694 g, 4.47 mmol) at rt. The reaction mixture was stirred at rt for 20 min. To the mixture was then added 1-(piperazin-1-yl)ethanone (0.572 g, 4.47 mmol) and the reaction mixture was stirred at rt for 1 h. The reaction was quenched with a saturated aqueous solution of NaHCO3 and extracted with CH2Cl2. The organic layer was washed twice with brine, dried by passing through a phase separating cartridge and evaporated. Purification by Flash chromatography using Biotage Isolera system (amine functionalized silica KP-NH, eluting with Cyclohexane/EtOAc 0 to 100%) gave the title compound (1.20 g, 68% yield) as a beige foam. MS: 457.4-459.3 [M+1]+, Rt(2′)=1.03 min., 13889-98-0

The synthetic route of 13889-98-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NOVARTIS AG; COOKE, Nigel Graham; FERNANDES GOMES DOS SANTOS, Paulo Antonio; FURET, Pascal; HEBACH, Christina; HOGENAUER, Klemens; HOLLINGWORTH, Gregory; KALIS, Christoph; LEWIS, Ian; SMITH, Alexander Baxter; SOLDERMANN, Nicolas; STAUFFER, Frederic; STRANG, Ross; STOWASSER, Frank; TUFFILLI, Nicola; VON MATT, Anette; WOLF, Romain; ZECRI, Frederic; US2015/342951; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

A suspension of 4-(4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (Step 8.3) (1.26 g, 4.1 mmol) and palladium on carbon (200 mg) in MeOH (30 ml.) was stirred for 30 min at rt, under a hydrogen atmosphere. The reaction mixture was filtered through a pad of celite and concentrated to afford 1.1 g of the title compound as a pink solid: ESI-MS: 278.2 [M+H]+; tR= 2.85 min (System 1 )., 182618-86-6

182618-86-6 1-Boc-4-(4-Nitrophenyl)piperazine 3380696, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NOVARTIS AG; WO2009/141386; (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.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.

(0413) To a solution of Compound 3J (90 mg), Compound 130C (64.2 mg), triethylamine (0.077 ml), N,N-dimethylpyridin-4-amine (38.5 mg) in a mixture of dichloromethane (5 ml) and N,N-dimethylformamide (0.5 ml) was added N1-((ethylimino)methylene)-N3,N3-dimethylpropane-1,3-diamine, hydrochloric acid (60.4 mg) and the mixture was stirred 18 hours. This was concentrated on high vacuum and the crude was purified by reverse phase chromatography with ammonium acetate buffer/acetonitrile. 1H NMR (500 MHz, pyridine-d5) delta 13.03 (s, 1H), 9.27 (d, 1H), 8.59 (d, 1H), 8.43 (d, 1H), 8.37 (dd, 1H), 8.11 (d, 1H), 7.65-7.67 (m, 2H), 7.44 (d, 2H), 7.07 (d, 2H), 6.88 (d, 1H), 6.76 (dd, 1H), 6.54 (d, 1H), 6.48 (m, 1H), 4.06 (m, 1H), 3.98 (d, 2H), 3.35 (t, 2H), 3.07 (m, 4H), 2.73-2.80 (m, 4H), 2.68-2.72 (m, 1H), 2.36 (q, 1H), 2.11-2.30 (m, 9H), 1.97 (m, 2H), 1.62-1.71 (m, 3H), 1.48-1.58 (m, 2H), 1.39 (t, 2H), 0.94 (s, 6H)., 1235865-77-6

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 66713100, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

548762-66-9, To a stirred solution of 64 mg (0.3 mmol) tert-butyl (25,5R)-2,5-dimethylpiperazine-1- carboxylate in 2 mL DOE were added at RT 160 pL DIPEA (0.9 mmol, 3 eq) and 86 mg 4-methylbenzenesulfonyl chloride (0.45 mmol, 1.5 eq) and the mixture was stirred overnight at RT. The organic phase was washed three times with water, dried andevaporated to yield 110 mg (100%) of the crude title compound which was used in the next step without further purification.[C-MS (Method 1): Rt = 1.39 mm; MS (ESIpos): m/z = 369 [M÷H]

As the paragraph descriping shows that 548762-66-9 is playing an increasingly important role.

Reference：
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; (74 pag.)WO2018/114672; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-34-8, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A. 4-(4-Amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester. 4-(2-Fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (4.0 g, 12.3 mmol), was dissolved into EtOH (200 ml.) and Pd/C 10% (300 mg) was added carefully. The resulting mixture was stirred under hydrogen atmosphere provided by hydrogen balloon for 24 h. The catalyst was removed and the concentration of the filtrate yield the title compound.MS (ESI) mass calculated for C15H22FN3O2, 295.35; m/z measured, 296.5 [M+H]+1H NMR (CDCI3): 6.76 (t, J = 9.2, 1 H), 6.44-6.35 (m, 2H), 3.62-3.49 (m, 6H), 2.93-2.82 (m, 4H), 1.47 (s, 9H).

154590-34-8, 154590-34-8 tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate 16203508, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); 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

N-(4-(2-(Chloromethyl)-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-7-yl)p (for a preparation see Intermediate 82, 50 mg, 0.151 mmol) was dissolved in DMF (5 mL), potassium carbonate (62.5 mg, 0.452 mmol) was added, followed by 1-methylpiperazin-2-one (17.20 mg, 0.151 mmol). The mixture was stirred for 3 h at room temperature. The mixture was diluted with water (10 mL) and extracted with a mixture of methanol (3 mL) and DCM (15 mL), the organic layer was dried, 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; AMANS, Dominique; BAMBOROUGH, Paul; BARKER, Michael David; BIT, Rino Antonio; BROWN, John Alexander; CAMPBELL, Matthew; GARTON, Neil Stuart; LINDON, Matthew J; SHIPLEY, Tracy Jane; THEODOULOU, Natalie Hope; WELLAWAY, Christopher Roland; WESTAWAY, Susan Marie; WO2014/140077; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

A solution of 2,4-dichloro-5,7-difluoro-3-nitroquinoline (5.58 gm, 2.0×10?2 moles) in 2-methyl tetrahydrofuran (50 mL) is stirred as diisopropylethylamine (2.84 gm, 2.2×10?2 moles) and N-2-aminoethyl-N? methylpiperazine (3.15 gm, 2.2×10?2 moles) are added. This solution is stirred at room temperature overnight. The yellow reaction mixture is diluted with more 2-methyl-tetrahydrofuran (50 mL) and this is washed with water (100 mL) followed by brine (50 mL). After being dried over magnesium sulfate, the solution is filtered and the solvent is removed under reduced pressure. The oily residue is stirred with diethyl ether (25 mL) and this is cooled on ice causing the product to crystallize. The solid yellow product is isolated by filtration, washed with ether and dried. The yield is about 4.32 gm.

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; JANUS BIOTHERAPEUTICS, INC.; Lipford, Grayson B.; Zepp, Charles M.; (72 pag.)US9873694; (2018); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Bubbled N2 through a suspension of 6-(4-bromophenyl)pyrazolo[l,5-a]pyrimidine (1.14 g, 4.16 mmol) (WO 2009/114180 Al, 2009) and (3R,5S)-tert-butyl 3,5-dimethylpiperazine-l- carboxylate (2.25 g, 10.50 mmol) in toluene (16 mL). Added bis(tri-t- butylphosphino)palladium (0) (0.106 g, 0.208 mmol) then sodium 2-methylpropan-2-olate (0.600 g, 6.24 mmol). Heated in 100 degree bath under N2. After 5 h, removed solvent. Partitioned between EA and water. Filtered through Celite, washing with ethyl acetate. Washed org layer with brine, dried (Na2S04), filtered and concentrated. Purified on Biotage (50 g) eluting with 25-75% EA/hex. Solid obtained from later peak was triturated in EtOH and filtered to obtain (3R,5S)-tert-butyl 3,5-dimethyl-4-(4-(pyrazolo[l,5-a]pyrimidin-6- yl)phenyl)piperazine-l-carboxylate (0.234 g, 0.574 mmol, 13.81 % yield) as a faint yellow solid.

129779-30-2, 129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; THE BRIGHAM AND WOMEN’S HOSPITAL, INC.; THE U.S.A., AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH & HUMAN SERVICES; ALIMARDANOV, Asaf; CUNY, Gregory, D.; GREWAL, Gurmit, Singh; LEE, Arthur; MCKEW, John, C.; MOHEDAS, Agustin, H.; SHEN, Min; XU, Xin; YU, Paul, B.; WO2014/160203; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics