Month: March 2021

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,76003-29-7

Step A1, 1 -dimethylethyl 4-[2~fluoro~4-(methyloxy)phenyl]-3-oxo-1-piperazinecarboxylate A mixture of 1-Boc-3-oxopiperazine (500 mg, 2.497 mmol), 4-bromo-3- fluoroanisole (512 mg, 2.497 mmol), copper(l) iodide (23.78 mg, 0.125 mmol), frans-Nu,Nu’- dimethylcycIohexane-1 ,2-diamine (0.039 mL, 0.250 mmo.), and potassium carbonate (690 mg, 4.99 mmol) in 1 ,4-dioxane (10 mL) was heated at 120 C for 3.5 days. The mixture was filtered through a pad of Celite and washed with EtOAc (50 mL). The filtrate was washed with saturated aqueous NH4CI (15 mL), brine (15 mL), dried ( gS04), filtered and concentrated. The crude was absorbed on silica gel and purified by silica gelchromatography (10-60% EtOAc in hexanes) to give 1 ,1 -dimethylethyl 4-[2-fluoro-4- (methyloxy)phenyl]-3-oxo~1 -piperazinecarboxylate (581.9 mg, 1 .794 mmol, 72 %) as white solid. MS(ESI) m/z: 325.3 (MH+).

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; MAYNARD, Andy; MILLER, John; PATTERSON, Dan; PEAT, Andrew, James; POWERS, Jeremiah; PRICE, Daniel, J.; ROBERTS, Chris; TAI, Vincent; YOUNGMAN, Michael; WO2011/50284; (2011); 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.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.

4-Cyclopropylmethyl-piperazine-1-carboxylic acid 4-(2-cyclohexyl-acetylamino)-phenyl Ester The title compound was prepared from 4-(2-cyclohexyl-acetylamino)-phenyl chloroformate and 1-cyclopropylmethyl-piperazine, preparative HPLC (methode C (60%, off-white crystals). HPLC-MS m/z=400.3 (M+1), Rt: 2.42 min., 57184-25-5

The synthetic route of 57184-25-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); 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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

tert-butyl 3,3-dimethylpiperazine-1-carboxylate (19.90 g, 92.86 mmol) and (2,2- dimethylpiperazin-1-yl)methanone hydrochloride (Intermediate C) (27.87 g, 84.60 mmol) are dissolved in DMF (300 mL) before HATU (35.45 g, 93.23 mmol) and DIPEA (27.72 g, 37.36 mL, 214.5 mmol) are added. The solution is stirred at room temperature for 3h, and then water is added dropwise. The aq. phase is extracted three times with EtOAc. The combined organic phase is washed with water and brine. The organic phase is then dried over Na2SO4, filtered and the filtrate evaporated under reduced pressure. The crude product is purified passing through a pad of silica gel (25%-33% EtOAc/hexanes affording the title product (34.28 g, 91% yield) as a yellow orange foamy solid, which is used directly in the next step. 1H NMR (400 MHz, Chloroform-d) 6 7.34 (s, 1H), 7.06 (s, 1H), 3.84 (dd, J = 6.6, 4.8 Hz, 2H), 3.67 – 3.45 (m, 4H), 2.71 (tt, J = 10.3, 5.5 Hz, 1H), 1.85 – 1.77 (m, 4H), 1.77 – 1.71 (m, 1H), 1.57 – 1.51 (m, 2H), 1.49 (s, 9H), 1.49 (s, 9H), 1.43- 1.31 (m, 3H), 1.01 (s, 3H), 0.97 (s, 3H). ESI-MS m/z calc. 525.3567, found 526.61 (M+1) Retention time: 3.15 minutes using method A.

259808-67-8, The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; LIU, Bingcan; DORICH, Stephane; DE LESELEUC, Mylene; DUPONT-GAUDET, Kristina; JAMES, Clint, Alwyn; VAILLANCOURT, Louis; BEAULIEU, Marc-Andre; STURINO, Claudio; (236 pag.)WO2018/57588; (2018); A1;,
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57260-70-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-70-5,tert-Butyl 4-benzylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The mixture of haloalkyl-5-benzhydryl-1H-tetrazole, 10a(300 mg, 1 mmol), alkylpiperazine, 13a (264, 1.5 mmol), K2CO3(276 mg, 2 mmol), NaI (catalyst) and CH3CN (15 mL) was refluxed. After the completion, reaction mixture was cooled, filtered and concentrated. The obtained product was purified by column chromatographyon silica gel with n-hexane: EtOAc: MeOH (10:1.5:0.5)to obtain 2a (131 mg, 30%) as light brown liquid. Rf = 0.56 (n-hexane:EtOAc: MeOH = 2.5:1.5:1). 1H NMR (500 MHz, CDCl3): d 7.35-7.24 (m, 15H), 5.84 (s, 1H), 4.72-4.69 (m, 2H), 3.49 (s, 2H), 3.04-2.97 (m, 2H), 2.53-2.42 (m, 8H); 13C NMR (125 MHz, CDCl3): d167.7, 140.9, 138.0, 129.2, 128.8, 128.6, 128.2, 127.1, 127.0, 63.0,56.4, 52.9, 52.8, 50.5, 48.6.

As the paragraph descriping shows that 57260-70-5 is playing an increasingly important role.

Reference£º
Article; Paudel, Suresh; Acharya, Srijan; Yoon, Goo; Kim, Kyeong-Man; Cheon, Seung Hoon; Bioorganic and Medicinal Chemistry; vol. 25; 7; (2017); p. 2266 – 2276;,
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.

Cat. TsOH monohydrate was added to a suspension of methyl 14′-cyclohexyl-2,2- dimethylspiro[l,3-dioxane-5,7′-indolo[l,2-e][l,5]benzoxazocine]-H’-carboxylate in MeOH/THF 1:2 (0.03 M), and the solution was stirred at RT for 3 h. Filtration on a pad of neutral alumina using EtOAc as eluent afforded after evaporation of the solvent in vacuo methyl 14-cyclohexyl- 7, 7-bis(hydroxymethyl)-7,8-dihydro-6H-indolo[l,2-e][l,5]benzoxazocine- 11 -carboxylate (quant). This material was dissolved in dry MeCN (0.2M) and DIPEA (4.0 eq) and trifluoromethane sulfonic anhydride (3.5 eq) was added at 0 0C. The mixture was stirred at 0 0C for 15 min, then more DIPEA (4 eq) was added at RT. 7ert-butyl 4-(2-aminoethyl)piperazine-l- carboxylate (2 eq) was added, and the mixture was stirred at 70 0C for 1 h. After removal of the solvent in vacuo EtOAc was added, the solution was washed with H2O and brine, dried over Na2SO4 and the solvent was removed in vacuo. The crude methyl \-{2-[4-(tert- butoxycarbonyl)piperazin- 1 -yljethyl} – 14′-cyclohexylspiro[azetidine-3 ,7′-indolo[ 1 ,2- e][l,5]benzoxazocine]-l l’-carboxylate was taken in DCM/TFA 3:1 (0.13M) and stirred at RT for 2 h. The mixture was evaporated to dryness and the residual material was dissolved in EtOAc. The solution was washed with sat. aq. NaHCO3 and brine. The organic phase was dried overNa2SO4 and the solvent evaporated in vacuo. The residue was dissolved in dry dioxane (0.06M) and sulfamide (5 eq) was added. The mixture was stirred at reflux for 3 h, then overnight at RT. The residue obtained after evaporation was purified by FC (EtOAc/MeOH, 9:1) to afford the title compound in 40percent yield. (ES+) m/z 622 (M+H)+., 192130-34-0

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

Reference£º
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI SPA; WO2009/10783; (2009); A1;,
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Piperazines – an overview | ScienceDirect Topics

5464-12-0,5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Sodium hydride, 60percent dispersion in mineral oil (252 mg, 6.29 mmol) was added, portionwise, to an ice-cooled solution of 2-(4-methyl-piperazin-l-yl)-ethanol (863 mg, 5.99 mmol) and 2-chloro-5- nitropyridine (1.0 g, 6.29 mmol) in DMF (20 ml). The ice-cooling was removed after 1 hour and the mixture was allowed to stir at rt overnight. The reaction mixture was added to ice/water and subsequently extracted with EtOAc (x2). The combined organic extracts were washed with water (x4) and brine (xl), dried and concentrated. The crude product was purified by flash column chromatography on silica gel (60 g) eluting with 10:1 DCM:MeOH to give the product as a brown oil (400 mg, 24percent). 1H NMR (400 MHz, DMSO-^6) delta ppm 2.13 (s, 3 H), 2.21 – 2.54 (m, 8 H), 2.70 (t, /=5.95 Hz, 2 H), 4.50 (t, J=5.95 Hz, 2 H), 7.04 (d, .7=9.16 Hz, 1 H), 8.47 (dd, 7=9.16, 2.75 Hz, 1 H), 9.07 (d, 7=2.29 Hz, 1 H); m/z (ES+APCI)+: 267 [M+H]+.

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; MEDICAL RESEARCH COUNCIL; WO2009/122180; (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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

5-Phenylpentanoic acid (105 mg, 0.59 mmol), HOBt (87 mg, 0.65 mmol), TBTU (208 mg, 0.65 mmol), anhydrous triethylamine (131 ??_, 0.94 mmol) and anhydrous 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 (150 mg, 0.65 mmol) and anhydrous 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 under nitrogen and monitored by TLC. After 24 hours, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M HCI solution. The aqueous mixture was extracted with DCM (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 the solvent removed in vacuo. The residue was purified using flash chromatography (3:2, EtOAc:n-hexane) to obtain the desired product in an 44 % yield. H NMR (300 MHz, CDCI3) ? 7.50-7.46 (m, 2H), 7.29- 7.14 (m, 5H), 6.91-6.87 (m, 2H), 3.74 (d, J = 4.5 Hz, 2H), 3.55 (d, J = 4.5 Hz, 2H), 3.20 (d, J = 3.6 Hz, 4H), 2.63 (d, J = 4.8 Hz, 2H), 2.35 (d, J = 4.8 Hz, 2H), 1.68 (d, J = 4.5 Hz, 4H). 3C NMR (75 MHz, CDCI3) 171.5, 152.9, 142.1 , 128.4, 128.3, 126.4 (q, J = 3 Hz), 125.8, 120.6 (q, J = 33 Hz), 1 19.2 (q, J = 271.5 Hz), 1 14.9, 48.3, 48.1 , 45.1 , 41.1 , 35.7, 33.1 , 31.1 , 24.8. MS (+ESI) calcd for C22 H25 F3 N2 O m/z: [M + Na]+, 413.181 1 ; found 413.1794 [Diff(ppm) = – 4.08].

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.

57184-25-5, To a solution of 4-(dibenzylamino)cyclohexan-1-one (273, 5 g, 17.0 mmol) and 1- (cyclopropylmethyl)piperazine (276, 2.4 g, 17.1 mmol) in DCM (30 mL) was added HOAc (1 mL). NaHB(OAc)3 (20 g, 94.4 mmol) was then added in portions. After stirring at room temperature for 48 h, the reaction mixture was neutralized with saturated sodium bicarbonatesolution and extracted with DCM (50 mL x 3). The combined organic phases were dried over Mg504 and concentrated in vacuo. The resulting residue was purified by column chromatography to afford (1 r,4r)-N,N-dibenzyl-4-(4-(cyclopropylmethyl)piperazin- 1- yl)cyclohexan-1-amine (277, 670 mg, 1.6 mmol) and (ls,4s)-N,N-dibenzyl-4-(4- (cyclopropylmethyl)piperazin- 1 -yl)cyclohexan- 1-amine (278, 1.2 g, 2.9 mmol).(1R,4R)-N,N-Dibenzyl-4-(4-(cyclopropylmethyl)piperazin- 1-yl)cyclohexan- 1-amine(277): ?H NMR (300 MHz, CDC13): 37.29-7.26 (m, 4H), 7.24-7.18 (m, 4H), 7.15 -7.10 (m,2H), 3.53 (s, 4H), 2.81- 2.60 (m, 6H), 2.44 – 2.36 (m, 2H), 2.29 (d, J= 6.6 Hz, 2H), 1.96 – 1.88(m, 4H), 1.58 – 1.29 (m, 4H), 1.21 – 1.10 (m, 2H), 0.88 – 0.77 (m, 1H), 0.50 – 0.42 (m, 2H),0.10-0.02 (m, 2H).(1S,4S)-N,N-Dibenzyl-4-(4-(cyclopropylmethyl)piperazin- 1-yl)cyclohexan- 1-amine(278): ?H NMR (300 MHz, CDC13): oe 7.29-7.27 (m, 4H), 7.23 -7.18 (m, 4H), 7.14-7.09 (m,2H), 3.57 (s, 4H), 2.96 – 2.49 (m, 8H), 2.40 (d, J= 6.6 Hz, 2H), 2.20 (s, 1H), 1.89 – 1.85 (m,2H), 1.77 – 1.66 (m, 2H), 1.48 – 1.44 (m, 2H), 1.26 – 1.17 (m, 3H), 1.00 – 0.82 (m, 1H), 0.55 -0.49 (m, 2H), 0.16-0.11 (m, 2H).

57184-25-5 1-(Cyclopropylmethyl)piperazine 965875, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; G1 THERAPEUTICS, INC.; STRUM, Jay, Copeland; JUNG, David; (250 pag.)WO2018/5860; (2018); 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.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

A solution of 1- (piperazin-1-yl) ethan-1-one (3.59 g, 28 mmol) and potassium carbonate (3.88 g, 28 mmol) were added to N, N-dimethylformamide (40 mL)Then 4-fluoro-2-methoxy-1-nitrobenzene (4.09 g, 23 mmol) was added to the suspension and stirred at 80 C overnight. The mixture was poured into water, The solid precipitate was filtered off. The resulting solid was dried in vacuo at 50 C, A yellow solid (3.5 g, yield: 45%)

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

Reference£º
Patent; Fudan University; Shanghai Institute of Materia Medica, Chinese Academy of Sciences; Li, Yingxia; Ding, Jian; Xiao, Qiang; Geng, Meiyu; Liu, Jian; Xie, Hua; (24 pag.)CN106608868; (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.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

N4-(5-Isopropyl-1H-pyrazol-3-yl)-N6-[2-(4-methylpiperazin-1-yl)ethyl]-N2-(3-phenylisoxazol-5-ylmethyl)-pyrimidine-2,4,6-triamine. A mixture of 6-chloro-N4-(5-isopropyl-1H-pyrazol-3-yl)-N2-(3-phenylisoxazol-5-ylmethyl)-pyrimidine-2,4-diamine (250 mg, 0.611 mmol) and 2-(4-methylpiperazin-1-yl)-ethylamine (500 mg, 3.50 mmol) in 1-butanol (2 mL) was heated to 180¡ã C. in a 50 mL sealed tube. The mixture was heated for 1 h, then cooled to room temperature and diluted with methanol (10 mL). The mixture thus obtained was purified via preparative reverse phase HPLC to give the desired product (93 mg, 29percent) as a white solid.1H-NMR (400 MHz, d6-CDCl3): delta 7.8 (m, 2H), 7.4 (m, 3H), 6.5 (s, 1H), 5.9 (s, 1H), 5.2 (s, 1H), 4.8 (m, 2H), 3.5 (br s, 2H), 2.8 (m, 1H), 2.5 (m, 10H), 2.4 (s, 3H), 1.2 (m, 6H); MS (I) for C27H36N10O: 517.3 (MH+)., 934-98-5

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

Reference£º
Patent; EXELIXIS, INC.; US2008/249079; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics