Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

55121-99-8, General Procedure for Synthesis of Examples 8 – 42; EPO EPO EPO The starting pyrimidyl chloride (54 mg, 0.15 mmol) was placed in a 2-5 mL microwave reaction vessel from Personal Chemistry, suspended in iPrOH (2 mL), and treated with concentrated HCI (0.075 mL) and an aniline monomer (0.3 mmol). The vial was sealed and the reaction was heated in the Smith Synthesizer at 170 0C for 20 minutes. The cap was removed and Et3N (0.5 mL) and CH2CI2 (2 mL) were added. The solvent was evaporated and the residue purified by reverse phase mass directed prep HPLC [conditions: 4 x 20 mm Phenomenex Luna C18(2) 3 micron column, eluted with 10-100% Methanol (0.075% Formic Acid) / Water (0.1% Formic Acid), 3 minute gradient time, 4 minute run, 2 ml/minute]. The appropriate fractions were combined and concentrated to give the final products. Compounds with greater than 80% purity by peak area were submitted for screening and are shown in the table below.

55121-99-8 (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone 231408, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2007/18941; (2007); 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.1188265-73-7,tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

tert-butyl 3-(2-hydroxyethyl) piperazine-1-carboxylate (6.91 g, 30.0 mmol) and 5-(2-bromoacetyl)-4-methylisobenzofuran-1(3H)-one (6.73 g, 25 mmol) were dissolved in tetrahydrofuran (100 mL) then added Hunig?sbase (8.73 mL, 50.0 mmol) and stirred at RT overnight. The reaction was poured into brine and extracted with EtOAc(2x). The combined organic layer was dried over Na2SO4, filtered and evaporated to dryness. The crude productwas chromatographed through an ISCO Redi-Sep 330g column and eluted with 5% MeOH /DCM solvent systemto the title compound. LC-MS (IE, m/z): 419 [M + 1]+., 1188265-73-7

1188265-73-7 tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate 53407692, 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; (128 pag.)EP2744499; (2016); B1;,
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Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 2-chloro-5-trifluoromethylpyridine (2.34 g, 12.9 mmol, 1.0 equiv.), 2-methypiperazine (2.59 g, 25.8 mmol, 2.0 equiv.) and triethylamine (5.4 mL, 38.7 mmol, 3.0 equiv.) in toluene (20 mL) was sealed in a 50 mL of high pressure reaction tube. The reaction mixture was heated to 150 C. with stirring. After stirring at 150 C. for 20 hours, the reaction mixture was cooled to room temperature and then diluted with CH2Cl2 (200 mL). The organic mixture was washed with water (100 mL¡Á2), brine and then dried over Na2SO4. After filtration and removal of solvent, 3.05 g (96% yield) of the desired intermediate was obtained as a bright yellow solid, which was used without purification. 1H NMR (400 MHz, CDCl3), delta (ppm): 8.42 (m, 1H), 7.65 (dd, 1H), 6.66 (d, 1H), 4.26 (m, 2H), 3.14 (m, 1H), 2.94 (m, 3H), 2.60 (dd, 1H), 1. 18 (d, 3H)., 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (2005); 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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.,59878-57-8

(4-fluoro-3-carboxybenzyl) thieno [2,3-D] pyrimidine-2,4 (1H, 3H) -dione (0.21 g, 0.66 mmol), tripyrrolidinium bromide phosphonium hexafluorophosphate (PyBrOP, 0.46 g, 0.99 mmol), 1-cyclopropanecarbonylpiperazine (0.1 g, 0.66 mmol), N, N-diisopropylethylamine (DIPEA, 0.17 g, 1.32 mmol), Dichloromethane (5 mL) was added to the reaction flask and stirred at room temperature overnight. The reaction solution was added with methylene chloride (5 mL) Water (5 mL), extracted and the organic layer washed with water (3 mL), dried, filtered and concentrated to give the crude product. The crude product was purified by silica gel column chromatography (mobile phase CH2Cl2 / CH3OH 50/1) The final product, 1- (4-fluoro-3- (4-cyclopropylcarbonylpiperazine- 1 -carbonyl) benzyl) thieno [2,3- D] pyrimidine-2,4 (1H, 3H) dione (I-2), a white solid (0.19 g, yield 63.3%),

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Patent; Shanghai Xunhe Pharmaceutical Technology Co., Ltd.; Zheng Yongyong; Jin Hua; Zhou Feng; Huang Meihua; Meng Xin; (28 pag.)CN107286174; (2017); 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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

3-(2-Furyl)propanoic acid (54 mg, 0.39 mmol), HOBt (58 mg, 0.43 mmol), TBTU (138 mg, 0.43 mmol), anhydrous triethylamine (87 ??, 0.63 mmol) and dry DMF (2 ml) were placed in an oven-dried Schlenk tube under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. A second Schlenk tube was prepared containing 1-(4-trifluoromethyl phenyl) piperazine (100 mg, 0.43 mmol and dry DMF (1 ml) under a nitrogen atmosphere. The resulting solution was stirred until complete dissolution of the piperazine had occurred. The piperazine solution was then transferred, via a cannula, to the first Schlenk tube containing the carboxylic acid. The resulting solution was stirred for 24 hrs, under nitrogen, and monitored by TLC. After 24 hrs, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M hydrochloric acid solution. The aqueous mixture was extracted with dichloromethane (20 ml, followed by 4 x 10 ml) and the organic layer washed with a saturated sodium bicarbonate solution (3 x 20 ml) and brine (3 x 20 ml). The organic layer was dried over magnesium sulphate and evaporated under reduced pressure. The residue was purified using flash chromatography (3:2, EtOAc:n-hexane) to obtain the desired product in an 31 % yield. H NMR (300 MHz, CDCI3) ? 7.48 (d, 2H), 7.31 (s, 1 H), 6.89 (d, 2H), 6.28 (t, 1 H), 6.04 (d, 1 H), 3.77 (t, 2H), 3.58 (t, 2H), 3.21-3.26 (m, 4H), 3.00 (t, 2H), 2.69 (t, 2H). MS (+ESI) calcd for C18 H19 F3 N2 02 m/z: [M + H]+ , 353.1471 ; found 353.1461 [Diff(ppm) = – 2.83].

30459-17-7, 30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH; STEPHENS, John; FINDLAY, John; KINSELLA, Gemma; MARTIN, Darren; DEVINE, Robert; VELASCO-TORRIJOS, Trinidad; WO2013/60860; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 69 (0.2 g, 0.57 mmol), 4-(2-amino-ethyl)-piperazine-l-carboxylic acidtert-butyl ester (0.26 g, 1.13 mmol) and DIEA (0.20 mL, 1.14 mmol) in 1-butanol (5 mL) washeated to 120¡ãC for 1.5 h. After concentration, the residue was purified by silica gelchromatography using 2-5percent MeOH/DCM, to give 4-[2-(5,6-diphenyl-furo[2,3-d]pyrimidin-4-ylamino)-ethyl]-piperazine-l-carboxylic acid tert-butyl ester 71 (0.20 g). Compound 71 wassubjected to 20 mL of 20percent TFA/DCM at rt for 2 h, then the reaction was concentrated almostto dryness under reduced pressure, and purified by silica gel column chromatography using0.1percent MeOH/DCM containing ImL ammonium hydroxide, to give 72 (0.15 g). MS: 400.2(M+l). ‘HNMRtDMSO-dg) ppm 8.36 (s, 1H), 7.61-7.33 (m, 10H), 5.49 (t, 1H, J=4.48Hz),3.45 (dd, 2H, Jr=5.10Hz, J2=5.84Hz), 2.33 (t, 2H, J=5.80Hz), 2.13 (br, 4H), 1.95 (br, 1H)(note: some peaks overlapped with water peak in DMSO-de). ‘HNMR (CCla-d) ppm 8.43 (s,1H), 7.60-7.50 (m, 6H), 7.50-7.26 (m, 4H), 5.39 (t, 1H), 3.54 (dd, 2H, J^S.OSHz, J2=6.20Hz),2.73 (t, 4H, J=4.71Hz), 2.44 (t 2H, J=5.91Hz), 2.28 (br, 4H), 1,87 (br, 1H).

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

Reference£º
Patent; AMGEN INC.; WO2006/4658; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

23.5) delta-Chloro-thiophene^-carboxylic acid [(S)-3-(4-cyclopropyl-piperazin-1-yl)-2-(2- methoxy-3-pyridin-4-yl-benzenesulfonylamino)-3-oxo-propyl]-amide hydrochloride Intermediate 82 (170 mg, 0.34 mmol) was dissolved in 10 ml DCM and N-cyclopropyl piperazine (134 mg, 0.38 mmol) was added followed by DIPEA (0.27 ml, 1.54 mmol) and TBTU (121 mg, 0.38 mmol). After 16 h stirring at RT, the solution was evaporated to dryness and purified by silica gel chromatography (Elution with DCM/methanol from 0 to 10% of methanol). The solid obtained after evaporation of the solvents was dissolved in DCM, HCI 2M in Et2O (5 ml) was added and the solvents were evaporated yielding a white powder. Yield: 112 mg, 50 % MS (ES+): m/e = 604.

20327-23-5, 20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SANOFI-AVENTIS; WO2009/103440; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5317-33-9, 3-(4-Methylpiperazin-1-yl)propan-1-ol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Di-tert-butyl azodicarboxylate (0.478 g, 2.08 mmol) was added portionwise to a mixture of product step 6 (1.66 mmol), the appropriate alcohol (1.74 mmol), and triphenyl-phosphine (0.544 g, 2.08 mmol) in dichloromethane (20 mL) at r.t. If necessary, further alcohol was added. After stirring for 2 h, the solution was concentrated to 10 mL, mounted on silica and chromatographed (gradient, dichloromethane to dichloromethane_methanol=3:2) to obtain the desired ethers (73%).The compound was synthesised according to GP 4 from 4-chloro-7-hydroxy-6-methoxy-quinazoline and 3-(4-methylpiperazin-1-yl)-propan-1-ol. LC/ESI-MS: m/z=351 [M+H]., 5317-33-9

5317-33-9 3-(4-Methylpiperazin-1-yl)propan-1-ol 79208, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; 4SC AG; US2006/135782; (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.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

To a mixture of 3-(4-chlorobenzoyl)propionic acid (31.9 g, 150 mmol), DMF (200 ml), and N-hydroxybenzotriazole (40.6 g, 301 mmol) was added a solution of N-ethyl-/V-(3-dimethylaminopropyl)carbodiimide hydrochloride (28.8 g, 150 mmol) in DMF (100 ml). The mixture was stirred at room temperature for 1.5 hour, and a solution of 1-cyclopentylpiperazine (23.2 g, 150 mmol) in DCM (100 ml) was added. The mixture was stirred at room temperature for 4 hours, concentrated under reduced pressure, and the residue was distributed between ethyl acetate (1.0 I) and a saturated, aqueous NaHCO3 solution (1.0 I). Phases were separated, the organic layer was dried (MgSO4), and concentrated, and the residue was redissolved in 1 molar aqueous hydrochloric acid (150 ml). The solution was concentrated, and the residue was dried by coevaporation with ethanol. Recrystallization of the residue from ethanol yielded 31.1 g (54%) of the title compound. Concentration of the mother liquor gave additional 19.4 g (34%) of product., 21043-40-3

As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference£º
Patent; Dorwald, Florencio Zaragoza; Andersen, Knud Erik; Sorensen, Jan Lindy; US2004/19039; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5271-27-2, 1-Methyl-3-phenylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5271-27-2, Example 119 and 120lambda/-Cyclopropyl-4-methyl-3-[3-(4-methyl-2-phenyl-1-piperazinyl)-2-oxo-1(2H)- pyrazinylj-benzamide (Example 119) and 3-[5-bromo-3-(4-methyl-2-phenyl-1 – piperazinyl)-2-oxo-1(2H)-pyrazinyl]-lambda/-cyclopropyl-4-methyl-benzamide (Example 120).A mixture of 3-(3,5-dibromo-2-oxo-2/-/-pyrazin-1-yl)-4-methyl-benzoic acid, methyl ester (Example 1 b, 1 15 mg), 1-methyl-3-phenyl-piperazine (77 mg), lambda/,lambda/-diisopropylethylamine (0.1 mL) and tetrahydrofuran (1 mL) was heated within a microwave for 30 minutes at 100¡ãC before being cooled to room temperature. The mixture was transferred to a mixture of palladium on carbon (10percent, 50 mg) and tetrahydrofuran (1 mL) and 1 ,4-cyclohexadiene (1 mL) was added. The mixture was heated under atmosphere of nitrogen within a microwave for 2.5 h at 120¡ãC. An additional portion of palladium on carbon (50 mg) in tetrahydrofuran (1 mL) was added and the mixture was heated for 1 h at 120¡ãC. After cooling, cyclopropylamine (0.3 mL) was added followed by dropwise addition of a solution of /so-propylmagnesium chloride (2M in tetrahydrofuran, 2.5 mL). The mixture was stirred for 10 min. and quenched with sat. aqueous NH4CI and extracted into ethyl acetate. The organic phase was dried (Na2SO4), filtered and concentrated. Purification by preparative HPLC (Gemini column, 0.1 percent ammonia: acetonitrile eluent) afforded lambda/-cyclopropyl-4- methyl-3-(4-methyl-3′-oxo-2-phenyl-3,4,5,6-tetrahydro-2/-/,3’/-/-[1 ,2′]bipyrazinyl-4′-yl)- benzamide (49 mg) and 3-(6′-Bromo-4-methyl-3′-oxo-2-phenyl-3,4,5,6-tetrahydro-2/-/,3’/-/- [1 ,2′]bipyrazinyl-4′-yl)-lambda/-cyclopropyl-4-methyl-benzamide (8 mg).lambda/-Cyclopropyl-4-methyl-3-[3-(4-methyl-2-phenyl-1-piperazinyl)-2-oxo-1(2H)- pyrazinylj-benzamideMS: APCI(+ve) 444 (M+H+).1H NMR .5(DMSO-Cl6, 400MHz) 8.45 (1 H, m), 7.88-7.83 (1 H, m), 7.75 and 7.71 (1 H, 2 x d), 7.52 – 7.42 (3H, m), 7.37 – 7.28 (2H, m), 7.25 – 7.16 (1 H, m), 6.98 (2H, s), 6.17 and 6.07 (1 H, 2 x br s), 3.27 – 3.10 (1 H, m), 2.90 – 2.70 (2H, m), 2.48 – 2.37 (2H, m), 2.20 (3H, m), 2.15 (2H, m), 2.1 1 and 2.04 (3H, 2 x s), 0.69 (2H, m), 0.55 (2H, m).3-[5-Bromo-3-(4-methyl-2-phenyl-1-piperazinyl)-2-oxo-1(2H)-pyrazinyl]-lambda/- cyclopropyl-4-methyl-benzamideMS: APCI(+ve) 522 (M+H+). 1H NMR 5(DMSO-Cl6, 400MHz) 8.42 (1 H, m), 7.85 (1 H, m), 7.77 and 7.74 (1 H, 2 x d), 7.52 – 7.41 (3H, m), 7.37 – 7.28 (2H, m), 7.27 – 7.19 (2H, m), 6.28 and 6.16 (1 H, 2 x br s), 3.29 (3H, s), 3.18 – 3.03 (1 H, m), 2.89 – 2.72 (2H, m), 2.48 – 2.36 (1 H, m), 2.20 (3H, m), 2.15 and 2.07 (3H, 2 x s), 0.69 (2H, m), 0.55 (2H, m).

The synthetic route of 5271-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/1132; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics