Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

According to scheme I, to a 250-mL flash were added Compound Ia-1, i.e. 2,6-dichloro-3,5-dimethoxyaniline (10mmol) and AcOH (24ml), and added dropwisely under an ice-bath a solution of sodium nitrite (15mmol) in sulphuric acid (5.8ml) . The mixture was stirred at 25C until the solution became clear. The resulting dark yellow solution was poured into 150ml of an ice-water, and urea (6mmol) was added. The mixture was stirred and filtered. An aqueous solution of potassium iodide (15mmol) was added to the above dark-yellow solution. The mixture was heated at 85C for 2 hours, and cooled to room temperature. NaHSO3 (3.4 mmol) was added, and the mixture was stirred for 10 minutes. The resulting yellow solid was filtered, dried, and separated by column chromatography to produce Compound Ib-1 (8mmol). Compound Ib-1 (4 mmol), and Compound A-1, i.e. 4-piperidinone ethylene ketal (6 mmol) were dissolved in 50ml toluene, and palladium acetate (0.4 mmol), BINAP (0.48 mmol), and cesium carbonate (18 mmol) were added. The mixture was refluxed under the nitrogen protection for 3 days, and separated by column chromatography to produce Compound Ic-1. Compound Ic-1 (2.5 mmol) was dissolved in 10ml THF, and 10% aqueous H2SO4 solution (10ml) was added. The mixture was heated at 60C overnight, and separated by column chromatography to produce Compound Id-1. Compound Id-1 (1.0 mmol) was dissolved in 10ml dioxane, and DMF.DMA (6.0 mmol) and triethylamine (1.0 mmol) were added. The mixture was refluxed under the nitrogen protection for 2 days, and separated by thin layer chromatography to produce Compound Ie-1. Compound B-1, i.e., 1-fluoro-4-nitrobenzene (10 mmol) was dissolved in 20ml DMF, and C-1, i.e., N-ethylpiperazine (11 mmol), and potassium carbonate (30 mmol) were added. The mixture was reacted at 70C overnight. After cooling, the mixture was poured into ice-water, and filtered to produce Compound If-1. Compound If-1 (10 mmol) was dissolved in 20ml methanol or ethanol, and palladium/carbon (1mmol) was added. The mixture was hydrogenated at room temperature for 7 hours. The mixture was separated by column chromatography to produce Compound Ig-1. Compound Ig-1 (2.6 mmol) was dissolved in 10ml dioxane, and cyanoamine (2.73 mmol), and concentrated hydrochloric acid (3.9 mmol) were added. The mixture was stirred under reflux overnight to produce Compound Ih-1. Compound Ie-1 (1mmol) and Compound Ih-1 (1.05mmol) were dissolved in 8ml ethanol, and sodium acetate (2mmol) and triethylamine (1.05mmol) were added. The mixture was stirred under flux for 7 hours, ethanol concentrated, and water and dichloromethane were added. The organic phase was separated, dried over anhydrous sodium sulphate, and separated by thin layer chromatography to produce Compound I-1 (0.1mmol) in a yield of 10%.H1-NMR(deuterated MeOH) : delta8.11(s, 1H), delta7.56(d, 2H), delta6.99(d, 2H), delta6.72(s, 1H), delta4.25(s, 2H), delta3.93(s, 6H), delta3.56(t, 2H), delta3.23(m, 4H), delta2.92(t, 2H), delta2.8(m, 4H), delta2.64(m, 3H), delta1.2(t, 3H). ESI(+)m/z: 543, 115619-01-7

The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shanghai Allist Pharmaceutical and Medical Technology Corporations; KUANG, Rongren; (39 pag.)EP3466948; (2019); 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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

Compound 6 (200 mg, 0.43 mmol), N-Cbz-piperazine (113 mg, 0.52 mmol), DhbtOH (81 mg, 0.49 mmol) were dissolved in DMF (3 ml) under argon at 0 ¡ãC. DCC (106 mg, 0.52 mmol) in DMF (0.5 ml) was added. The reaction was stirred at 0 ¡ãC for 1 h and then at room temperature overnight. The DCU precipitate was removed by filtration. The crude mixture was purified by flash chromatography on a Flasmaster II using an Isolute propylene disposable flash column and the following gradient: EtOAc/hexane 0:100–>50:50 and then CHCl3/MeOH 100:0–>90:10 to yield the title compound as a yellow wax (233 mg, 81percent). Rf = 0.2 (5percent MeOH in CH2Cl2); 1H NMR (500 MHz; CDCl3) delta 9.82 (s, 1H, NH), 7.66-7.29 (m, 16H, H-Ar and CHN), 5.60 (d, 1H, J = 7.7 Hz, CHCO), 3.77-3.25 (m, 13H, CH2CH2OSi, CHCH2N, CH2CHCH, 4 x CH2CH2N), 1.85-1.67 (m, 2H, CH2CH2CH), 1.04-0.94 (s, 9H, (CH3)3C); 13C NMR (125 MHz; CDCl3) delta 171.2 (C), 164.1 (C), 154.0 (C), 150.8 (C), 146.2 (CH), 136.3 (C), 135.5 (C), 133.0 (C), 130.3 (C), 128.3 (C), 128.1 (C), 127.8 (C), 101.3 (CH), 68.1 (CH2), 61.5 (CH2), 51.8 (CH2), 45.4 (CH2), 41.8 (CH2), 36.6 (CH), 33.4 (CH2), 26.9 (CH3), 19.1 (C); LRMS (ES+) m/z 669.3 [M+H]+; HRMS (ES+) found 669.3128 [M+H]+, inlMMLBox requires 669.3157., 31166-44-6

31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Baragan?a, Beatriz; McCarthy, Orla; Sa?nchez, Paula; Bosch-Navarrete, Cristina; Kaiser, Marcel; Brun, Reto; Whittingham, Jean L.; Roberts, Shirley M.; Zhou, Xiao-Xiong; Wilson, Keith S.; Johansson, Nils Gunnar; Gonza?lez-Pacanowska, Dolores; Gilbert, Ian H.; Bioorganic and Medicinal Chemistry; vol. 19; 7; (2011); p. 2378 – 2391;,
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.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

A mixture of (4-Trifluoromethyl-phenyl)-acetic acid (0.14 g, 0.63 mmol), 4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (0.15 g, 0.52 mmol), TBTU (0.20 g, 0.63 mmol) and DIPEA (0.11 mL, 0.63 mmol) in15 anhydrous DMF (3 mL) was stirred at r.t. overnight. The reaction was poured in a saturated solution of NaHC03 andextracted with EtOAc (2 x 15 mL), the organic phase was washed with brine, dried with anhydrous Na2S04 andevaporated under vacuum. The crude was purified by flash column chromatography (DCM/MeOH 97/3) to obtain thetitle compound (0.25 g, 80%) as white solid.1H NMR (600 MHz, DMSO-dG) o ppm 0.99 (br. s., 3 H) 2.17- 2.48 (m, 8 H) 3.58 (s, 2 H) 7.73 (d, J=8.42 Hz, 1 H)20 7.81 (dd, J=9.25, 1.37 Hz, 1 H) 7.85 (dt, J=7.97, 2.06 Hz, 1 H) 8.00-8.05 (m, 2 H) 8.17 (d, J=2.02 Hz, 1 H) 10.61 (s,1 H)., 630125-91-6

630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.

Reference£º
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl (3R)-3-(hydroxymethyl)piperazine-l-carboxylate (5.00 g, 23.12 mmol, 1.00 eq) in ethyl acetate (50 mL) and water (50 mL) was added sodium bicarbonate (5.83 g, 69.00 mmol, 3.00 eq) in one portion, then benzyl carbonochloridate (5.94 g, 35.00 mmol, 1.51 eq) was added to the solution slowly with stirring at 0 C for 30 minutes. The resulted solution was stirred at 10 C for 5 hours. The organic layer was separated from the reaction solution, and washed with water (10 mL). The aqueous phase was extracted with ethyl acetate (100 mL). The organic layer was collected and combined, washed with water (30 mL x 3) brine (30 mL), dried over sodium sulfate, concentrated under reduced pressure to give a yellow liquid. The yellow liquid was purified by silica gel column chromatography (Petroleum ether/Ethyl acetate = 3/1 to 1/1) to obtained compound Ol-benzyl-04-tert-butyl (2R)-2-(hydroxymethyl)piperazine- l,4-dicarboxylate (8.00 g, 22.83 mmol, 99% yield) as colorless liquid. 1H-NMR (400MHz, CDCL) d 7.33 – 7.24 (m, 5H), 5.08 (s, 2H), 4.18 (br s, 1H), 3.87 (br s, 2H), 3.57 (br s, 2H), 3.12 – 2.78 (m, 2H), 1.97 (s, 2H), 1.60 – 1.57 (m, 1H), 1.40 (s, 9H)., 278788-66-2

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARVINAS OPERATIONS, INC.; YALE UNIVERSITY; CREW, Andrew P.; HORNBERGER, Keith R.; WANG, Jing; DONG, Hanqing; BERLIN, Michael; CREWS, Craig M.; (1213 pag.)WO2019/195609; (2019); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

5-(Oxiran-2-yl)-2-benzofuran-l(3H)-one (1.5 g, 8.5 mmol) and commercially available (5)-4-N-BOC-2-hydroxymethyl piperazine (2.394 g, 11.07 mmol) were combined in ethanol (10 mL) in a microwave tube. The mixture was degassed then heated for 60 min at 150 C. LC-MS showed the product peak. The reaction was worked up by adding ethyl acetate and washing once with brine. The organic layer was separated, dried, and concentrated to dryness. The crude product was purified by MPLC using an 80g Redi-sep column and eluted with 50%- 100% EtOAc/ hexane yielding the title compound., 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; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound MH3-3 (284.2mg, 0.8mmol) was dissolved in DMSO (5.0mL) was added TEA (0.2mL, 1.44mmol) and Compound S1-5 (259.5mg, 1.2mmol), microwave at 90 deg.] C of The reaction 12h, cooled to room temperature, dichloromethane (15 mL), then washed three times (15 mL), dried over anhydrous white solid was recrystallized from ethanol to give 243.8mg, 55.26%, 1030377-21-9

As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference£º
Patent; Guangdong Zhong Hospital; Guangdong Experiment Animal Monitor Suo; Liu Bo; Xu Guangyu; Yu Jie; Wu Yue; Chen Cha; Xu Fangfang; Zhang Yu; Han Xiaodong; Lin Dongling; Huang Ren; Lu Jinjian; Zhang Yuqin; (62 pag.)CN106674254; (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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of 1, 1-dimethylethyl (2S)-2-methyl-1-piperazinecarboxylate (Intermediate 26,100 mg, 0.5 mmol) in CH2CI2 (5 mL) was mixed with 3-bromo benzaldehyde (0.06 mL, 0.5 mmol) and NaB (OAc) 3H (0.16 g, 0.75 mmol). The resulting mixture was stirred for 12 hours, diluted with dichloromethane (30 mL) and washed with brine (50 mL). The organic layer was collected, dried over Na2SO4 and concentrated. Separation via a combiflash system then afforded the title compound (150 mg, 81%). LC/MS : m/z, 369 (M+H) ;’HNMR (MeOD) 1.26 (3H, d), 1.47 (9H, s), 2.0 (1H, m), 2.1 (1H, m), 2.6 (1H, m), 2.8 (1H, m), 3.1 (1H, m), 3.3 (2H, s), 3.4 (1 H, m), 3.5 (1 H, m), 3.8 (1 H, m), 4.2 (1 H, m), 4.88 (1 H, s), 7.25 (1 H, m), 7.3 (1 H, m), 7.4 (1 H, m), 7.55 (1 H, s)., 169447-70-5

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2005/87236; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 9 (2-Iodo-5-methanesulfonyl-phenyl)-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-methanone To a solution of 2-Iodo-5-methanesulfonyl-benzoic acid (Example C, 3.0 g, 9.2 mmol) in dimethylformamide (20 ml) were successively added TBTU (3.8 g, 11.5 mmol), N-ethyldiisopropylamine (8.0 ml, 46.0 mmol) and 1-(4-trifluromethylphenyl)piperazine (ABCR F07741NB, [30459-17-7], 2.5 g, 11.0 mmd). The reaction was then stirred at room temperature for two hours, then concentrated in vacuo and purified by column chromatography (SiO2, 50 g, CH2Cl2/MeOH/NH3=100/0/0 to 95/4.5/0.5), to give the title compound as a pale brown foam; MS (m/e): 539.1 (M+H+). TBTU=2-(1 H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Patent; Alberati-Giani, Daniela; Jolidon, Synese; Narquizian, Robert; Nettekoven, Matthias Heinrich; Norcross, Roger David; Pinard, Emmanuel; Stalder, Henri; US2005/59668; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

848482-93-9, (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (S)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (500 mg, 2.171 mmol) in 1,4-dioxane (5 mL) and water (20 mL) was added potassium carbonate (1200 mg, 8.69 mmol) followed by (9Hfluoren-9-yl)methyl carbonochloridate (562 mg, 2.171 mmol) at 0 C. The mixture was stirred at RT for 18hrs and then treated with water (10 ml). The resulting mixture was extracted with diethyl ether (2¡Á15 ml).The aqueous phase was acidified with aq. HCl (1M) to pH 2-3, and extracted with DCM (3¡Á20 ml). Thecombined organic layers were dried over MgSO4 and concentrated to give the crude product. The crudeproduct was purified via prep HPLC (10-100% CH3CN:Water with 0.1% TFA buffer) to afford the product(S)-1-(((9H-fluoren-9-yl)methoxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (294 mg,30% yield) as a white solid. 1H NMR (500 MHz, methanol-d4) d 7.83 (t, J=6.6 Hz, 2H), 7.68-7.58 (m,2H), 7.45-7.38 (m, 2H), 7.38-7.30 (m, 2H), 4.65 (br. s., 1H), 4.58 (d, J=13.7 Hz, 1H), 4.55-4.39 (m, 3H),4.33-4.18 (m, 1H), 2.91-2.85 (m, 4H), 1.47 (s, 9H). ESI-MS(+) m/z=475 (M+Na)., 848482-93-9

848482-93-9 (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid 1501850, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Bristol-Myers Squibb Company; Miller, Michael Matthew; Mapelli, Claudio; Allen, Martin Patrick; Bowsher, Michael S.; Boy, Kenneth M.; Gillis, Eric P.; Langley, David R.; Mull, Eric; Poirier, Maude A.; Sanghvi, Nishith; Sun, Li-Qiang; Tenney, Daniel J.; Yeung, Kap-Sun; Zhu, Juliang; Reid, Patrick C.; Scola, Paul Michael; (892 pag.)US9308236; (2016); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

848482-93-9, (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of octanal (0.68 mL, 4.3 mmol) in tetrahydrofuran (2 mL) was added to a stirred solution of (S)-piperazine-l , 3-dicarboxylic acid 1-tert-butyl ester (1.0 g, 4.3 mmol) in tetrahydrofuran (1 15 mL). Acetic acid (0.9 mL, 15.8 mmol) was added to the solution. After stirring the reaction mixture for 30 minutes, sodium triacetoxyborohydride (1.37 g, 6.5 mmol) was added in portions over 5 minutes and the mixture stirred for 18h. The mixture was then filtered through Celite and the filtrate evaporated to an oil (1.47 g). The oil was stirred with diethyl ether (20 mL) and the insoluble solid was filtered off and purified by column chromatography over silica gel, eluting with a gradient of methanol/ethyl acetate to give the title compound as a white solid (287 mg, 0.84 mmol, 19%), m/z 343 (MuEta ‘ ). C18H34N2O4 exact mass 342.25., 848482-93-9

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

Reference£º
Patent; NEW PHARMA LICENCE HOLDINGS LIMITED; BROWN, Pamela; DAWSON, Michael; SIMONOVIC, Mona; BOAKES, Steven; DUPERCHY, Esther; STANWAY, Steven James; WILSON, Antoinette; MOSS, Stephen Frederick; WO2015/135976; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics