Month: May 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Example 15.1.2: Preparation of 4-[2-(2-Amino-benzoimidazol-l-yl)-ethyl]- piperazine-1-carboxylic acid tert-butyl ester; 4-[2-(2-Amino-benzoimidazol-l-yl)-ethyl]-piperazine-l-carboxylic acid tert-butyl ester was prepared according to the procedure described in WO2005/058869. 1H NMR (300MHz, CDCl3): delta 7.43 (IH, d, J = 7.5 Hz, Ar-CH), 7.17-7.06 (3H, m, Ar- CH), 5.78 (2H, s, NH2), 3.64 (2H, t, J = 5.7 Hz, NCH2CH2N), 3.46 (4H, m, CH2NCH2), 2.56 (4H, m, CH2NCH2), 2.43 (2H, t, J = 5.7 Hz, NCH2CH2N), 1.46 (9H, s, C[CH3J3). MS (ESI+) m/z 346 (M+ 1)., 208167-83-3

208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AVEXA LIMITED; WO2008/77188; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

892242-64-7, 4-((3-(4-Cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

892242-64-7, About 21kg of 4-((3-(4-cyclohexylpiperazin-l-yl)-6-oxo-6H-anthra[l,9- cd]isoxazol-5-yl)amino)benzoic acid was slurred in 625L of 0.4 M NaOH in MeOH and purified water (4: 1) solution under about 40-45C for about 2-4 hours. Then slowly cooled the reaction to room temperature and stirred for another 2-4 hours. After confirmed the reaction completion by HPLC, the solid was centrifuged and washed with about 57L of MTBE. The wet cake was re- suspended in about 245L of 0.1M NaOH in MeOH/H20 solution under room temperature. The wet cake was centrifuged and washed with about 56L of MTBE again. The filtered solid was re- suspended in about 250L of MTBE under room temperature for about 1-2 hours. The solid was separated and dried at 25-30C under reduced pressure for 12-24 hours to obtain the final product with purity more than 99.9% (HPLC) and about 90% yield. Mass spectra give [M+l] = 523.2. 1H-NMR (400 MHz, DMSO-d6, see Figure 1), ppm (delta): 11.79 (IH, s), 8.48 (IH, d), 8.20 (IH, d), 7.93 (2H, d), 7.84 (IH, t), 7.72 (IH, t), 7.35 (2H, d), 6.39 (IH, s), 3.85 (4H, m), 2.72- 2.70 (4H, m), 2.28-2.265 (IH, m), 1.72-1.78 (4H, m), 1.55-1.58 (IH, m), 1.08-1.23 (5H, m). Sodium content: 3.8%. The Raman spectrum is shown in Figure 4, and the XRPD data is given in Table 1 below and Figure 2, IR spectra is given in Figure 5 and DSC spectra is given in Figure 3. These data confirm the stable crystalline polymorphic form (Form A) of the compound of Formula I.

The synthetic route of 892242-64-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PURDUE PHARMA L.P.; WU, Jay Jie-Qiang; WANG, Ling; (31 pag.)WO2017/27465; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0209] Step 1. To a solution of N-(l-(lH-indol-3-yl)hexan-2-yl)-2-bromothiazole-5- carboxamide (0.10 g, 0.24 mmol) and 4-methylpiperazin-2-one (0.03 g, 0.29 mmol) in dioxane (7 mL), Cs2C03 (0.23 g, 0.72 mmol) and 2-(dicyclohexylphosphino)3,6-dimethoxy-2′,4′,6′- triisopropyl-l,l’-biphenyl (BrettPhos precatalyst; 0.02 g, 0.02 mmol) were added. The reaction vessel was purged with argon for 20 min and the mixture was then heated at 110 C for 16 h. The reaction mixture was filtered through diatomaceous earth, washing with 5% MeOH in DCM (2 x 10 mL). The filtrate was concentrated, and the crude obtained was purified by column chromatography (silica, 100-200 mesh, 1 to 4% MeOH in DCM) and preparative HPLC to afford the title compound (0.03 g, 14%) as a white solid. HPLC Purity: 99.4%; MS (ESI) m/e [M+H]+/Rt/%: 440.00/2.69/98.0%; 1H NMR (400 MHz, DMSO-d6) delta 0.81 (t, 7 = 6.8 Hz, 3H), 1.19-1.35 (m, 4H), 1.47-1.63 (m, 2H), 2.31 (s, 3H), 2.81 (t, 7 = 5.4 Hz, 2H), 2.85-2.97 (m, 2H), 3.34 (s, 2H), 4.03 (t, 7 = 5.6 Hz, 2H), 4.16 (m, 1H), 6.92-6.98 (m, 1H), 7.04 (t, 7 = 7.6 Hz, 1H), 7.11 (d, 7 = 1.5 Hz, 1H), 7.31 (d, 7 = 8.3 Hz, 1H), 7.58 (d, 7 = 7.8 Hz, 1H), 8.13 (s, 1H), 8.24 (d, 7 = 8.8 Hz, 1H), 10.75 (brs, 1H).

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NEUROPORE THERAPIES, INC.; WRASIDLO, Wolfgang; STOCKING, Emily, M.; HALL, Adrian; MACCOSS, Malcolm; (139 pag.)WO2017/20010; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

928025-56-3, (S)-tert-Butyl 3-ethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of Intermediate 13 (1 g, 4.61 mmol) in POCI3 (13 mL, 139.17 mmol) was added N,N-dimethylaniline (0.274 g, 2.26 mmol). The reaction mixture was heated at 110C for 6 h, then concentrated in vacuo. The solid obtained was triturated in pentane. To a stirred solution of the unpurified residue (1.3 g, 5.57 mmol) in THF (40 mL) were added triethylamine (6.43 mL, 46.15 mmol) and tert- butyl (3S)-3-ethylpiperazine-l -carboxylate (1.08 g, 5.08 mmol). The reaction mixture was stirred at r.t. for 12 h, then concentrated in vacuo. The residue was dissolved in EtOAc (50 mL). The organic layer was washed with water (50 mL), then dried over anhydrous sodium sulfate and concentrated in vacuo. The crude residue was purified by column chromatography (normal phase; silica gel: 100-200 mesh; 2% EtOAc in hexanes) to afford the title compound (0.62 g, 33%). deltaEta (CDC13, 400 MHz) 7.82 (s, 1H), 4.22-4.10 (m, 2H), 3.40-3.30 (m, 2H), 3.22-3.10 (m, 3H), 2.58 (s, 3H), 1.84-1.74 (m, 2H), 1.48 (s, 9H), 0.98-0.80 (m, 3H). LCMS (ES+) [M+H]+ 413.45, RT 4.20 minutes (method 4)., 928025-56-3

928025-56-3 (S)-tert-Butyl 3-ethylpiperazine-1-carboxylate 24820542, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; HORSLEY Helen Tracey; HUANG Qiuya; NEUSS Judi Charlotte; REUBERSON James Thomas; VANDERHOYDONCK Bart; WO2015/193169; A1; (2015);,
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.

General procedure: N-Cbz piperazine (0.55 g, 2.48 mmol, 1 eq) and carboxylic acid 8c?g (2.48 mmol, 1 eq) were dissolved in dry DMF (10 mL), the reaction mixture flushed with argon and cooled to 0 ¡ãC. N-methyl morpholine (NMM; 7.44 mmol,3 eq), hydroxybenzotriazole hydrate (HOBt; 2.98 mmol,1.2 eq) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimidehydrochloride HCl salt (EDC; 3.22 mmol, 1.3 eq) were slowly added. The reaction mixture was stirred under argon atmosphere for 5 h at 0 ¡ãC and an additional 15 h at room temperature. DMF was evaporated under reduced pressure and the residue redissolved in dichloromethane (10 mL).The dichloromethane phase was washed with H2O (1 x 10 mL), a 1 M HCl solution (3 x 10 mL), saturated aqueous NaHCO3 solution (3 9 10 mL), brine (1 x 20 mL), dried over Na2SO4, filtered, and the solvent evaporated under reduced pressure. The crude product was purified by flash column chromatography using ethyl acetate/hexane solvents as eluents to afford compounds 9c?g.

31166-44-6, As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Article; Juki?, Marko; Frlan, Rok; Chan, Fiona; Kirby, Robert W.; Madge, David J.; Tytgat, Jan; Peigneur, Steve; Anderluh, Marko; Kikelj, Danijel; Medicinal Chemistry Research; vol. 24; 6; (2015); p. 2366 – 2380;,
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.

31166-44-6, Into a 1 L round-bottom flask was placed benzyl piperazine-l-carboxylate (15 g, 68.10 mmol, 1.00 equiv), 4-(tetramethyl- l,3,2-dioxaborolan-2-yl)benzoic acid (16.9 g, 68.12 mmol, 1.00 equiv), EDC (14.4 g, 75.12 mmol, 1.10 equiv), HOBt (5.8 g, 42.92 mmol, 0.50 equiv), and triethylamine (27.6 g 272.75 mmol, 4.00 equiv) in dichloromethane (300 mL). The resulting solution was stirred for 18 h at RT. The mixture was then washed with 0.5M sodium carbonate (aq, 75 mL). The resulting mixture was then washed with 0.5M HC1 (aq, 75 mL) followed by 0.5M sodium carbonate (aq, 75 mL). The solution was concentrated in vacuo and the crude product was recrystallized from tBME/hexane (1: 1). This afforded the title compound (26 g, 84percent) as a white solid. LC-MS (ES, m/z): 451[M+H]+

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

Reference£º
Patent; FORMA THERAPEUTICS, INC.; BAIR, Kenneth, W.; LANCIA, David, R.; LI, Hongbin; LOCH, James; LU, Wei; MARTIN, Matthew, W.; MILLAN, David, S.; SCHILLER, Shawn, E.r.; TEBBE, Mark, J.; WO2014/164749; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

67455-41-8, 4-(Piperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,67455-41-8

Add 2-chloro-4-(cyclopentylamino) pyrimidine-5-carboxylic acid ethyl ester (1.3 g, 4.82 mmol) to an eggplant-shaped bottle containing 20 mL of isopropanol, and add Et3N (0.49 g, 4.82 mmol), 4-Piperazinyl aniline (1.11 g, 6.27 mmol), refluxed after the addition, after 6.0 hours TLC showed that the reaction was complete, and concentrated under reduced pressure to give the target crude product (1.31 g), CH2Cl2: MeOH = 20:1 to obtain pure product (1.06 g, 51.7%).

As the paragraph descriping shows that 67455-41-8 is playing an increasingly important role.

Reference£º
Patent; FIRST AFFILIATED HOSPITAL ZHENGZHOU UNIV; Zhengzhou University The First Affiliated Hospital; KAN QUANCHENG; Kan Quancheng; TIAN XIN; Tian Xin; ZHANG XIAOJIAN; Zhang Xiaojian; YANG ZHIHENG; Yang Zhiheng; DU YUE; Du Yue; CHENG WEIYAN; Cheng Weiyan; YUAN YONGLIANG; Yuan Yongliang; WANG SUHUA; Wang Suhua; (29 pag.)CN108299312; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 266 was prepared by the method indicated in the scheme belowusing well known synthetic procedures, 208167-83-3

As the paragraph descriping shows that 208167-83-3 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; JOHNSON & JOHNSON (CHINA) INVESTMENT LTD.; DAI, Xuedong; QUEROLLE, Olivier Alexis Georges; KROSKY, Daniel Jason; CAI, Wei; FU, Liqiang; KONG, Linglong; LIU, Yingtao; WAN, Zhao-Kui; HERKERT, Barbara; PANDE, Vineet; EDWARDS, James Patrick; PATRICK, Aaron Nathaniel; ANGIBAUD, Patrick Rene; PONCELET, Virginie Sophie; (488 pag.)WO2019/120209; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6,57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 121: tert-Butyl 4-(3-hvdroxypropyr)piperazine-l -carboxylate A mixture of tert-butyl piperazine-1 -carboxylate (2.75 g, 14.8 mmol), l-bromo-3- propanol (1.43 mL, 16.2 mmol) and potassium carbonate (2.25 mL, 27.5 mmol) in acetonitrile (75 mL) was heated at 950C for 4 hours. The solvent was removed under reduced pressure, and the residue was taken up in dichloromethane (300 mL) and washed with water, brine, EPO dried over sodium sulfate and concentrated under reduced pressure. Chromatography on silica gel with methanol in dichloromethane (0-10%) gave a tan solid 2.88 g (80% yield). MS (ESV 245 (MH+) for C12H24N2O3,1H-NMR TCDCl1) delta: 1.44 (m, 9H); 1.70-1.82 (m, 2H); 2.40-2.53 (m, 2H); 2.62-2.65 (m, 2H); 3.43-3.50 (m, 4H); 2.77 (m, 2H); 3.73-3.82 (m, 2H).

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

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/134378; (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.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,548762-66-9

Half of the solid from the previous step was treated with N,N-diisopropylethylamine (0.5 mL, 3 mmol), DMSO (0.5 mL, 7 mmol) and (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (273 mg, 1.27 mmol) and the reaction mixture was heated at 120 C. overnight, concentrated by rotary evaporation, dissolved in a small amount of DCM and purified by silica gel chromatography (0-50% ethyl acetate:hexanes) to produce the title intermediate (288 mg, 29% yield) as a yellow solid. (m/z): [M+H]+ calcd for C24H27F4N4O4 591.09; 593.09. found 593.2.

548762-66-9 (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate 11745988, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; LONG, Daniel D.; MCKINNELL, Robert Murray; JIANG, Lan; LOO, Mandy; LEPACK, Kassandra; VAN ORDEN, Lori Jean; OGAWA, Gavin; HUANG, Xiaojun; ZHANG, Weijiang; US2013/115194; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics