Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, To a stirred and cooled (0 C.) solution of 2-bromoacetyl bromide (1.72 mL, 19.8 mmol) in dichloromethane (25 mL) was added a solution of tert-butyl piperazine-1-carboxylate (7.75 g, 41.6 mmol) in dichloromethane (20 mL), dropwise over ?20 minutes. The cooling bath was then removed and the reaction was allowed to stir another two hours before transferring to a separatory funnel along with a dichloromethane rinse of the reaction flask (?30 mL). The solution was washed with 1.0 N hydrochloric acid (2*?50 mL) and aqueous sodium bicarbonate solution (1*?50 mL). The organic layer was dried (Na2SO4) and concentrated to afford title compound as a clear, faint amber gum (5.68 g, 93%). The crude intermediate was deemed sufficiently pure to use, without purification, in the next step. 1H NMR (400 MHz, CDCl3) delta 3.87 (s, 2H), 3.63-3.57 (m, 2H), 3.55-3.41 (m, 6H), 1.48 (s, 9H) ppm.

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GENZYME CORPORATION; LIM, Sungtaek; BARKER, JR., Robert H.; CROMWELL, Mary A.; MAKINO, Elina; HIRTH, Bradford; JIANG, John; MANIAR, Sachin; MUNSON, Mark; CHOI, Yong-Mi; THURAIRATNAM, Sukanthini; MUSICK, Kwon Yon; PRIBISH, James; ANGELASTRO, Michael; US2020/102324; (2020); 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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

4-Chloro-6-(3,4-dichloro-phenyl)-pyrimidine (0.1 lg, 0.4mmol) was added in one portion to a suspension of piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester (0.21g, 0.85mmol) and in fert-butanol (2ml) in a microwave reactor tube. The tube was sealed and heated to 150C in a microwave for 40 minutes at a pressure of 250psi. After this time the reaction mixture was cooled to room temperature and the solvent was removed. The resulting residue was purified by flash column chromatography (elution: 20% EtOAc, 80% Heptane) to give the title compound (0.36g, 75% yield) as a colourless oil. deltaEta (500 MHz, DMSO) 8.59 (s, 1 H) 8.43 (d, J=2.05 Hz, 1 H) 8.17 (dd, J=8.51, 2.05 Hz, 1 H) 7.74 – 7.81 (m, 1 H) 7.42 (d, J=7.88 Hz, 1 H) 4.88 – 5.09 (m, 1 H) 4.60 – 4.76 (m, 1 H) 4.24 – 4.46 (m, 1 H) 3.76 – 3.88 (m, 1 H) 3.56 (d, J=13.08 Hz, 3 H) 3.38 – 3.51 (m, 1 H) 3.10 – 3.28 (m, 2 H) 1.31 -1.47 (m, 9 H). Tr = 3.71 min m/z (ES+) (M+H+) 283, 285.

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; DOMINGUEZ, Celia; TOLEDO-SHERMAN, Leticia, M.; COURTNEY, Stephen, Martin; PRIME, Michael; MITCHELL, William; BROWN, Christopher, John; DE AGUIAR PENA, Paula, C.; JOHNSON, Peter; WO2013/16488; (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.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,655225-01-7

Intermediate 22: 1 ,1-Dimethylethyl 4-{2-r6-amino-2-(butyloxy)-8-(methyloxy)-9H- purin-9-yl1ethyl)-1-piperazinecarboxylate; 2-(Butyloxy)-8-(methyloxy)-9H-purin-6-amine trifluoroacetate (131 mg, 0.373mmole) and potassium carbonate (185mg, 0.41 mmole) in DMF (1 ml) was stirred and heated at 60¡ãC for 1 hour. A solution of 1 ,1-dimethylethyl 4-(2-bromoethyl)-1- piperazinecarboxylate (120mg, 0.41 mmole) in DMF (0.6ml) was added and the mixture stirred at 500C for 2.5 hours and then left at room temperature overnight. The mixture was heated at 500C for a further 4 hours and then quenched with water (10ml) and extracted with ethyl acetate (3×1 OmI). The combined organic extracts were dried over anhydrous sodium sulphate, filtered and evaporated. The residue was purified by silica gel chromatography eluting initially with chloroform:methanol 90:1 then 80:1 then 75:1 and finaly 60:1. Product-containing fractions were combined and evaporated to give the title compound as a yellow oily solid (168mg). 1H NMR (CDCI3): delta 5.66 (2H, d), 4.25 (2H, t), 4.05 (2H, t), 4.10 (3H, s), 3.35 (4H, broad s), 2.71 (2H, t), 2.46 (4H, broad s) 1.76 (2H, q) 1.48 (2H, q), 1.45 (9H, s) and 0.96 (3H, t).

The synthetic route of 655225-01-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; BAZIN-LEE, Helene; BIGGADIKE, Keith; COE, Diane, Mary; LEWELL, Xiao, Qing; MITCHELL, Charlotte, Jane; TRIVEDI, Naimisha; WO2010/18131; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

184042-60-2, 1-(2-Fluoroethyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 7-oxa-10,13,17,18,21 -pentaazatetracyclo[12.5.2.1A{2,6}.0A{17,20}]docosa- 1 (20),2,4,6(22),14(21 ),-15,18-heptaene hydrochloride (300 mg, 0.904 mmol) and diisopropylethylamine (616 muIota, 3.62 mmol) in tetrahydrofuran (2.5 ml) and N,N-dimethylformamide (2.5 ml) was added drop wise to a solution of di(imidazol- 1 -yl)methanone (220 mg, 1 .356 mmol) in tetrahydrofuran (1 .5 ml). The mixture was stirred at room temperature for 2 hours. 1 -(2-Fluoroethyl)piperazine hydrochloride (229 mg, 1 .36 mmol) was added and the reaction mixture was stirred at 80 C for 63 hours and at 1 10C for 24 hours. Di(imidazol-1 -yl)methanone (150 mg, 0.904 mmol) was added and the mixture was stirred at 1 10 0 C for 18 hours. The solvent was removed under reduced pressure and the residue was purified by reversed phase HPLC (HPLC method A). The product fractions were collected and the solvent was removed under reduced pressure. The product was taken up in dichloromethane/methanol (4:1 , 520 muIota) and 4N HCI in 1 ,4-dioxane (48 muIota, 0.191 mmol) was added. The reaction mixture was stirred at room temperature for 2 hours. The solvent was removed under reduced pressure and the compound was triturated with diethyl ether, filtered and dried under vacuum.Yield: 84 mg of example 17 (19%)LCMS method 2: MH+ = 454, RT = 2.032 min

184042-60-2, 184042-60-2 1-(2-Fluoroethyl)piperazine hydrochloride 22281452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; IPSEN PHARMA S.A.S.; ONCODESIGN S.A.; HOFLACK, Jan; BLOM, Petra; WO2013/46029; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-fluorobenzonitrile (0.041 mol, 5 g) in DMF (10 ml) were added K2C03 (0.082 mol, 11.4 g) and 1 -methylpiperazine (0.062 mol, 6.15 g). The mixture was stirred over 1 8h at 100C. The mixture was partitioned between water and ethyl acetate. The organic phase was washed with water and brine. The resulting solution was dried oversodium sulfate and evaporated to dryness. The title compound was obtained as a white solid and used without further purification (7 g, 84%).(ESI+) MS: m/z 202.3 (MHj., 109-01-3

As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Patent; EUDENDRON S.R.L.; UNIVERSITA’ DEGLI STUDI DI MILANO; ANGIOLINI, Mauro; ZUCCOTTO, Fabio; BERNARDI, Anna; AIRAGHI, Francesco; (144 pag.)WO2016/96709; (2016); 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.1284243-44-2,tert-Butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 2: 1-(4-fluorophenyl)piperazin-2-one To the solution of tert-butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate (2 g, 6.80 mmol) in dichloromethane (5 ml) was added slowly hydrogenchloride in 1,4-dioxane (16.99 ml, 68.0 mmol) at 0 C. and reaction was stirred for 3 h at 25 C. After completion of the reaction, the solvent was evaporated under reduced pressure to obtained salt was triturated with diethyl ether (2*10 ml) decanted it and dried to give 1-(4-fluorophenyl)piperazin-2-one hydrochloride (1.2 g, 5.20 mmol, 77%) 1H NMR (400 MHz, DMSO-d6) delta 9.90 (bs, 1H, D2O exchangeable), 7.38-7.34 (m, 4H), 3.85-3.72 (m, 4H), 3.55-3.50 (m, 2H). MS: m/z 195 (M+1).

1284243-44-2, As the paragraph descriping shows that 1284243-44-2 is playing an increasingly important role.

Reference£º
Patent; LUPIN LIMITED; Jana, Gourhari; Kurhade, Sanjay Pralhad; Jagdale, Arun Rangnath; Kukreja, Gagan; Sinha, Neelima; Palle, Venkata P.; Kamboj, Rajender Kumar; US2015/152118; (2015); 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.848482-93-9,(S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a round bottom flask equipped with a stir bar and charged with (S)-methyl 3-(m-tolyloxy)-2-(tritylamino)propanoate (8.28 g, 18.34 mmol) in MeOH (30 mL) and THF (30 mL) was added lithium hydroxide in water(55.0 mmol, 27.5 mL). The mixture was stirred at room temperature for 1 h. The reaction mixture wasneutralized with aq. 2N HCl. The mixture was diluted with EtOAc and the organic phase was isolated andwashed with brine; dried over MgSO4; filtered; then concentrated in vacuo. The resulting residue waspurified via silica gel chromatography to afford (S)-3-(m-tolyloxy)-2-(tritylamino)propanoic acid, 1.47 g(18%). 1H-NMR (400 MHz, CDCl3) delta 7.44 (d, J=7.1 Hz, 6H), 7.35-7.24 (m, 8H), 7.09 (t, J=7.8 Hz, 1H),6.76 (d, J=7.6 Hz, 1H), 6.52 (s, 1H), 6.46 (d, J=8.1 Hz, 1H), 4.07 (dd, J=9.2, 2.3 Hz, 1H), 3.71 (t, J=3.2 Hz,1H), 2.79 (dd, J=9.2, 4.0 Hz, 1H), 2.28 (s, 3H)., 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

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

694499-26-8, General procedure: To a solution of 3-iodo-4-methylbenzoyl chloride obtained above in dry DCM (10mL) at 0C was added Et3N (0.28mL, 2.0mmol) and 4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) aniline (328mg, 1.2mmol). The mixture was stirred at room temperature for 5h, and then the solvent was removed under reduced pressure. The residue was purified by using column chromatography to afford the corresponding product 6-1 (439mg, 2 steps yield: 85%).

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
Article; Liu, Yang; Peng, Xia; Guan, Xiaocong; Lu, Dong; Xi, Yong; Jin, Shiyu; Chen, Hui; Zeng, Limin; Ai, Jing; Geng, Meiyu; Hu, Youhong; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 122 – 132;,
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.

(1058) To a solution of Compound 3J (617 mg) and Compound 340A (386 mg) in dichloromethane (10 ml) was added 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide hydrochloride (288 mg) and 4-(dimethylamino)pyridine (183 mg). The mixture was stirred overnight. The mixture was diluted with dichloromethane (300 ml) and washed with aqueous NaHCO3, water, brine and dried over Na2SO4. Filtration and evaporation of the solvent gave the title compound.

1235865-77-6, The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.342405-34-9,4-(4-Methylpiperazino)benzyl Alcohol,as a common compound, the synthetic route is as follows.

A solution of 4-(4-formyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (1.3 g, 4.47 mmol) in THF (50 mL) was mixed with LAH (0.7 g, 17.87 mmol) and stirred at reflux for 14 h. The reaction was quenched at room temperature by adding KOH aqueous (14 N, 20 mL). The supernatant was decanted and combined with DCM washings, then diluted with water (50 mL). The mixture was extracted with DCM (3¡Á50 mL) followed by concentration using a rotary evaporator to give [4-(4-methyl-piperazin-1-yl)-phenyl]-methanol (0.82 g, 89%). To a solution of DMSO (0.56 mL, 7.96 mmol) in DCM (50 mL) at -78 C. was added oxalyl chloride (0.7 mL, 7.96 mmol) and the resulting mixture was stirred at -78 C. for 0.5 h. A solution of [4-(4-methyl-piperazin-1-yl)-phenyl]-methanol (0.82 g, 3.98 mmol) in DCM (20 mL) was slowly added. The reaction was stirred at -78 C. for 1.5 h. Triethylamine (1.7 mL, 11.94 mmol) was added and the reaction was allowed to gradually warm up to room temperature. After stirring for 4 h the reaction was quenched by adding sodium bicarbonate aqueous (1 N, 50 mL). The mixture was extracted with DCM (3¡Á50 mL) followed by concentration to afford a residue, which was further purified by column chromatography to yield 4-(4-methyl-piperazin-1-yl)-benzaldehyde (0.5 g, 61%).5,7-Dimethoxy-2-(4-(4-methylpiperazin-1-yl)phenyl)quinazolin-4(3H)-one was synthesized from 2-amino-4,6-dimethoxybenzamide and 4-(4-methyl-piperazin-1-yl)-benzaldehyde, using the method described for 5,7-dimethoxy-2-(pyridin-2-yl)quinazolin-4(3H)-one. 5,7-Dimethoxy-2-(4-(4-methylpiperazin-1-yl)phenyl)quinazolin-4(3H)-one (120 mg, 41%) was converted to the corresponding hydrochloride (a yellow solid). Selected data: MS (m/z): 381.11; MP 252.4-254.2 C. (di-hydrochloride).

342405-34-9, The synthetic route of 342405-34-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Wong, Norman C.W.; Tucker, Joseph E.L.; Hansen, Henrik C.; Chiacchia, Fabrizio S.; McCaffrey, David; US2008/188467; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics