Tag: M.W:200-300

848482-93-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.848482-93-9,(S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

(S)-4-Boc-2-piperazinecarboxylic acid (530 mg, 2.17 mmol) was dissolved in MeOH (25 mL) and formaldehyde (1.76 mL, 37 wt % in water, 21.7 mmol) was added. The reaction mixture was stirred for 30 min, NaBH(OAc)3 (0.92 g, 4.34 mmol) was added and the reaction mixture was stirred for 2 h. The solvents were removed in vacuo and the residue was purified by reverse phase column chromatography. The residue and benzyl homopiperazine (0.41 g, 2.17 mmol) were dissolved in DMF (20 mL) and cooled to 0 C. DIPEA (0.59 g, 4.56 mmol) and HBTU (0.82 g, 2.17 mmol) were added and the reaction mixture was stirred for 3 h. The solvents were removed in vacuo and the residue was partitioned between DCM (100 mL) and water (50 mL). The organic fraction was washed with 1M aq Na2CO3 (25 mL), brine (25 mL), dried (MgSO4) and concentrated in vacuo. The residue was purified by reverse phase column chromatography to give the title compound (0.64 g, 71%) as a light yellow gum. LCMS (ES+): 417.4 [MH]+.

The synthetic route of 848482-93-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Proximagen Limited; Savory, Edward Daniel; Stewart, Allson; Cartey, Allison; Brown, Giles; Simpson, Iain; Oliver, Kathryn; Patient, Lee; Higginbottom, Michael; Cole, Andrew Graham; US2013/289020; (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.187669-60-9,1-(4-(Methylsulfonyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 77; 4-{2-[4-(4-Methanesulfonylphenyl)piperazin-l-yl]ethylidene}piperidine-l- carboxylic acid tert-butyl ester; To a solution of 4-(2-hydroxyethylidene)piperidine-l-carboxylic acid tert-butyl ester (2.2g, 9.7mmol) in DCM (25mL) was added Et3N (2.02mL, 14.5mmol) and the reaction cooled to O0C. To this cooled mixture was added methanesulfonylchloride (0.98mL, 12.6mmol) dropwise. The reaction was stirred at O0C for 20 min then treated with saturated NaHCO3 solution. The two layers were separated and the organic layer washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by flash chromatography with 10% EtOAc / Hexane as eluent to afford 4-(2-chloroethylidene) piperidine-1-carboxylic acid tert-butyl ester and 4-vinyl-3,6-dihydro-2H-pyridine-l-carboxylic acid tert-butyl ester in a 1:1 ratio (0.95Og). The mixture was dissolved in DMF (5mL) and treated with TBAI (0.068g, 0.18mmol). This suspension was thus added to a preformed mixture of l-(4-methanesulfonylphenyl)piperazine (0.487g, 2.03mmol) and sodium hydride (0.1 Ig of a 60% dispersion in mineral oil, 2.77mmol) in DMF (5mL) at rt. The mixture was allowed to stir for 2h then treated with water. The aqueous was extracted with EtOAc and the combined organic layers washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by HPLC to afford the title compound (0.27g, 6%): RT = 2.41 min; m/z (ES+) = 450.2 [M+ H]+, 187669-60-9

As the paragraph descriping shows that 187669-60-9 is playing an increasingly important role.

Reference：
Patent; PROSIDION LIMITED; WO2007/3964; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

To a suspension of triphosgene (0.21 g, 0.71 mmol) and Na2C03 (0.45 g, 4.27 mmol) in DCM (18 ml), kept at 0 ocunder argon, 4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (0.61 g, 2.13 mmol) was added. Thereaction was monitored by HPLC (following the formation of 4-ethyl-piperazine-1-carboxylic acid [4-(4-ethylpiperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-amide by treating a sample of the reaction mixture with N-25 ethylpiperazine). After 1 h, 3-ethynyl-phenylamine (0.26 g, 2.18 mmol) was added and the reaction was let understirring overnight at r.t.. The mixture was diluted with DCM, washed with water (3 x 10 ml), dried over anhydrousNa2S04 and concentrated under vacuum. Purification by flash column chromatography (DCM/MeOH 95/5) affordedthe product as yellow solid (0.64 g, 70%).1H NMR (600 MHz, DMSO-dG) o ppm 0.95-1.00 (m, 3 H) 2.22-2.47 (m, 10 H) 3.52 (s, 2 H) 4.14 (s, 1 H) 7.09 (d,30 J=7.69 Hz, 1 H) 7.30 (t, J=7.88 Hz, 1 H) 7.41 (dd, J=8.24, 1.28 Hz, 1 H) 7.56 (dd, J=8.61, 1.83 Hz, 1 H) 7.61 – 7.64(m, 1 H) 7.66 (t, J=1.65 Hz, 1 H) 7.95 (d, J=2.01 Hz, 1 H) 8.85 (s, 1 H) 9.02 (s, 1 H).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference：
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; MENICHINCHERI, Maria; ANGIOLINI, Mauro; BERTRAND, Jay Aaron; CARUSO, Michele; POLUCCI, Paolo; QUARTIERI, Francesca; SALOM, Barbara; SALSA, Matteo; ZUCCOTTO, Fabio; WO2014/72220; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

7-Bromo-1H-indole-2-carboxylic acid (1) (2.4 g, 10 mmol), 4-((4-methylpiperazin-1-)methyl)-3-(trifluoromethyl)aniline(2.73g, 10mmol) and 2-(7-oxobenzotriazole)-N,N,N’,N’-tetramethyluronium hexafluorophosphate (HATU)(3.8 g, 10 mmol) dissolved in N,N-dimethylformamide,Diethylisopropylamine (1.65 mL, 10 mmol) was added.Stir until the reaction is complete, extract with ethyl acetate and water,The organic phase was concentrated and subjected to column chromatography to give 3.5 g of product, yield 70%., 694499-26-8

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Beijing Seth Ming Qiang Pharmaceutical Technology Co., Ltd.; Zhang Qiang; Zhang Hongbo; Zhou Likai; Feng Shouye; Yang Hailong; Wang Zhongxiang; (54 pag.)CN109988151; (2019); A;,
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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(a) 4-Chloro-2-methoxy-N-[2-(1-piperazinyl)ethyl]benzamide trifluoroacetate A solution of 4-chloro-2-methoxybenzoyl chloride (2.1 g), tert-butyl 4-(2-aminoethyl)-1-piperazinecarboxylate (3.0 g) and triethylamine (2.6 ml) in dichloromethane (100 ml) was stirred at room temperature for 72 hours. The solution was washed with brine, dried and treated with trifluoroacetic acid. After 16 hours the solution was concentrated and the residue triturated under ether to give the product as an oil (4.1 g).

192130-34-0, As the paragraph descriping shows that 192130-34-0 is playing an increasingly important role.

Reference：
Patent; Astrazeneca UK Limited; US6562825; (2003); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5747-48-8, A solution of but-3-yn-2-one (1 mmol) and PDBTZ (1 mmol), in ethyl acetate (10 mL) is refluxed for two hours. The reaction mixture is washed (water, brine), dried (sodium sulfate), and evaporated. The crude material is purified by flash chromatography to provide the enamine product.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; WO2008/79847; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At 0 deg.C, to pentafluorophenol in 520mL of anhydrous ether solution were added in portions 49g 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide (286mmol) and 12mL formic acid (312mmol). The batch was stirred at ambient temperature for 2 hours. Then add 32g 1-tert-butyl 3-methyl 1,3-piperazindicarboxylate (130mmol) and 18mL triethylamine (130mmol) dissolved in 520mL CH2Cl2 mixture. The batch was stirred at ambient temperature overnight. 1N HCl was hydrolyzed with an aqueous solution of the reaction mixture was extracted with CH2Cl2. The organic phases were then combined, then washed with saturated aqueous NaHCO3, and then washed with a saturated aqueous solution of NaCl until neutrality. Dried over MgSO4, filtered and concentrated to dryness, purified product (petroleum ether / AcOEt gradient: 0-30%) by silica gel chromatography. To give the title product as an oil.

129799-08-2, The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Les Laboratoires Servier; Vernalis (R&D) Limited; Le Tiran, A.; Le Diguarher, T.; Starck, J-B.; Henlin, J-M.; De Nanteuil, G.; Geneste, O.; Davidson, J.E.P.; Murray, J.B.; Chen, I-J.; (57 pag.)CN105579450; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

303-26-4, 1-((4-Chlorophenyl)(phenyl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1 : Preparation of5-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-l-yl)-N-(4-methylbenzyl)-3-meth yl-5-oxopentanamide; [147] [148] 0.5 mmol of 4-(4-methylbenzylcarbamoyl)-3-methylbutanoic acid prepared inPreparative Example 1, 0.55 mmol of l-(4-chlorobenzhydryl)piperazine, and ben- zotriazol-1-yloxytripyrrolidino phosphonium hexafluorophosphate (PyBOP) were added to 3 mL of dimethylformamide (DMF) to dissolve. Then, 1.0 mmol of N,N-diisopropylethylamine (DIEA) was added thereto, and stirred at room temperature for 16 hours. 20 mL of 10% HCl was put into the reaction solution, and extracted with 30 mL of EtOAc. The organic layer was washed with 20 mL of 10% HCl, and then washed with 20 mL of a saturated NaHCO solution twice and with 20 mL of a saturated NaCl solution twice. The organic layer was collected, dried over anhydrous MgSO 4 , and filtered under reduced pressure. The organic solvent in the filtrate was removed under reduced pressure. The residue was purified by column chromatography with a mixed solvent of EtOAc and methanol (20:1), so as to obtain the title compound (light yellow solid, yield: 65%).[149] mp 62-630C;[150] 1U NMR (CDCl ) delta 7.35 (d, J=8.0 Hz, 2CH), 7.29 (d, J=7.2 Hz, 2CH), 7.26 (t, J=8.2 Hz, 2CH), 7.22 (t, J=7.3 Hz, CH), 7.16 (d, J=8.0 Hz, 2CH), 7.11 (d, J=7.2 Hz, 2CH), 6.29 (s, NH), 4.37 (d, J=5.6 Hz, CH2), 4.21 (s, CH), 3.59 (t, J=5.6 Hz, CH2), 3.48 (q, J=5.6 Hz, CH2), 2.43 (d, J=6.8 Hz, CH2), 2.34-2.39 (m, CH2), 2.32 (s, CH3), 2.28 (d, J=6.0 Hz, CH ), 2.25 (d, J=6.4 Hz, CH ), 2.13-2.23 (m, CH), 1.03 (d, J=6.4 Hz, CH3);[151] HR-FABMS Calcd for C H ClN O : (M++l): 518.2574, Found: 518.2584.31 36 3 2

303-26-4, As the paragraph descriping shows that 303-26-4 is playing an increasingly important role.

Reference：
Patent; PARK CHOO, Hea-Young; WO2007/142431; (2007); A1;,
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,129779-30-2

Sodium triacetoxyborohydride (0.32 g, 1 .51 mmol) was added to a solution of tert-butyl (3R,5S)-3,5-dimethylpiperazine-i -carboxylate (0.28 g, 1 .30 mmol) and 4-[2-(dimethyl amino)ethoxy]benzaldehyde (Preparation 18a, 0.25 g, 1.29 mmol) in dichloromethane (10 mL) and the resulting mixture was stirred at room temperature for 4 days. The reaction mixture was washed with 2M aqueous solution of sodium hydroxide and theorganic layer was separated, dried over magnesium sulfate and the solvent evaporated to dryness. 4M Solution of hydrochloric acid in 1,4-dioxane was added to the residue and the resulting mixture was stirred at room temperature for 2 hours. The solvent was evaporated to dryness to yield the hydrochloride salt of the title compound (299 mg, 45%) as a solid.LRMS (mlz): 292 (M+i).

The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ALMIRALL, S.A.; BACH TANA, Jordi; PEREZ CRESPO, Daniel; LLERA SOLDEVILA, Oriol; ESTEVE TRIAS, Cristina; TABOADA MARTINEZ, Lorena; WO2015/86693; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

4-Methanesulfonyl-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 10 mmol of Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester were dissolved in 20 ml methylenchloride. 1.05 eq of DIPEA and mesylchloride were added. The reaction mixture was stirred at room temperature for 30 min. The product was extracted from etylacetate/water. The crude material was redissolved in methanol and treated with 2N NaOH. The reaction mixture was stirred at room temperature for 2 h. The mixture was neutralized with HCl and the product isolated via extraction from ethylacetate/water. MS(ISO): 307.4 (M-H+), 129799-15-1

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference：
Patent; Ackermann, Jean; Bleicher, Konrad; Ceccarelli Grenz, Simona M.; Chomienne, Odile; Mattei, Patrizio; Schulz-Gasch, Tanja; US2007/129544; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics