Month: August 2020

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.

General procedure: To a solution of acid (0.33mmol) in DMF (2mL), diisopropylethylamine (0.33mmol) and HATU (0.33mmol) were added. The mixture was left 33h stirring at room temperature and then the appropriate amine (0.45mmol) was added. After 16h at room temperature the solvent was removed under reduced pressure; the residue was dissolved in 2mL of DCM and washed with 2mL of 0.4N Na2CO3 solution. The organic layer was separated, dried over Na2SO4 and the solvent removed under reduced pressure.

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

Reference£º
Article; Nencini, Arianna; Pratelli, Carmela; Quinn, Joanna M.; Salerno, Massimiliano; Tunici, Patrizia; De Robertis, Alessandra; Valensin, Silvia; Mennillo, Federica; Rossi, Marco; Bakker, Annette; Benicchi, Tiziana; Cappelli, Federico; Turlizzi, Elisa; Nibbio, Martina; Caradonna, Nicola P.; Zanelli, Ugo; Andreini, Matteo; Magnani, Matteo; Varrone, Maurizio; European Journal of Medicinal Chemistry; vol. 95; (2015); p. 526 – 545;,
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.5521-39-1,2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

Example 39 6-Methoxy-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid {4-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-phenyl}-amide. This compound was prepared from 6-methoxy-8-(4-Methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid hydrochloride (Reference Example 2) and 2-[4-(4-amino-phenyl)-piperazin-1-yl]-ethanol (Reference Example 19) as prepared in Example 12, yielding a yellow solid. (80 mg=60%). mp=211.5-212.2 (dec.), MS-base peak at m/z=492 by positive ion and m/z=490 by negative ion CI

As the paragraph descriping shows that 5521-39-1 is playing an increasingly important role.

Reference£º
Patent; Chapdelaine, Marc; Davenport, Timothy; Haeberlein, Markus; Horchler, Carey; McCauley, John; Pierson, Edward; Sohn, Daniel; US2004/87575; (2004); 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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

A solution of l-methylpiperazin-2-one (40.8mg, 357 umol, 1.4 eq) and Compound D from Example 47 (0.10 g, 255.5 umol, 1.0 eq) in MeOH (10 mL) and DCE (10 mL) was adjusted to pH ~ 5 with AcOH and stirred for 1 hour. NaBH3CN (64.2 mg, 1.0 mmol, 4.0 eq) was added after which the mixture was stirred at 25¡ãC for 15 hours until there was no more starting material by LC/MS analysis. The mixture was quenched with sat.NaHCCb to pH=8 and then extracted with DCM (100 mL chi 3). The organic phases were combined and washed with brine (50 mL), dried over anhydrous Na2S04, filtered and concentrated under vacuum to give the crude product which was purified by prep-TLC(15: 1 DCM/MeOH) 3 times to give the desired product 323 (20 mg, 15 percent yield, 95percent purity) as a yellow solid. LC/MS (method 2): tR= 3.16 min, m/z (M + H)+ = 490.1. MR (400 MHz, CD3OD) delta 8.74 – 8.70 (m, 2H), 8.49 – 8.43 (m, 2H), 7.75 – 7.65 (m, 3H), 3.91 (s, 3H), 3.79 – 3.71 (m, 2H), 3.42 (t, J = 5.2 Hz, 2H), 3.35 (s, 2H), 3.00 – 2.92 (m, 5H), 2.83 (t, J= 11.2 Hz, 2H), 2.64 – 2.53 (m, 1H), 2.13 – 2.05 (m, 2H), 1.82 – 1.68 (m, 2H).

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; THE BRIGHAM AND WOMEN’S HOSPITAL, INC.; THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; YU, Paul, B.; HUANG, Wenwei; SANDERSON, Philip, Edward; JIANG, Jian-kang; SHAMIM, Khalida; ZHENG, Wei; HUANG, Xiuli; TAWA, Gregory; LEE, Arthur; ALIMARDANOV, Asaf; HUANG, Junfeng; (357 pag.)WO2018/200855; (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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of YL7-102 (8c, Scheme 3) (0.308 g, 0.8 mmol) and tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate (0.222 g, 0.8 mmol) in 2-propanol (4 mL) was heated at80 C in a sealed tube for 5 h. The resulting precipitate was filtered upon cooling, and washed with 2-propanol (2 mL x 3), then dried under high vacuum to afford the title compound as a light green solid (0.440 g, 83%). Mp.: 184-186 C; HPLC 99.8% (tR = 5.23 mm, 70% CH3OH in 0.1% TFA water, 20 mm); ?H NMR (400 MHz, DMSO-d6): oe 10.26 (brs, 1H disappear on D20 shake), 10.12 (brs, 1H disappear on D20 shake), 9.31 (brs, 1H disappear on D20 shake), 8.71 (s, 1H),7.51-7.33 (m, 4H), 7.02 (appd, J 6.0 Hz, 2H), 4.05-3.98 (m, 1H), 3.75-3.70 (m, 1H overlapping with water peak), 3.63-3.57 (m, 1H overlapping with water peak), 3.47-3.42 (m, 6H), 3.10 (brs, 4H), 1.96-1.88 (m, 1H), 1.83-1.76 (m, 2H), 1.56-1.48 (m, 1H), 1.40 (s, 9H); ?9F NMR (376 MHz, DMSO-d6): oe -116.16- -116.20 (m); LC-MS (ESI+) m/z 626.25; (M+H) HRMS (ESI+) m/z calculated for C3,H38C1FN704 (M+H) 626.2652, found 626.2651.

As the paragraph descriping shows that 170911-92-9 is playing an increasingly important role.

Reference£º
Patent; H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.; MAHAJAN, Nupam, P.; MAHAJAN, Kiran, N.; LAWRENCE, Nicholas, J.; LAWRENCE, Harshani, R.; WO2015/21149; (2015); 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

Palladium(ll) acetate (0.020 g, 0.090 mmol), 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (0.078 g, 0.135 mmol), 4-methylpiperazin-2-one (0.061 g, 0.540 mmol), cesium carbonate (0.440 g, 1 .350 mmol) and the title compound from Preparative Example 6 (0.120 g, 0.450 mmol) were added to a reaction vial followed by degassed 1 ,4-dioxane (5 ml). The vial was filled with argon gas and sealed and heated at 120 C for 45 minutes. The reaction mixture was cooled to room temperature and the residue was taken up with dichloromethane (40 mL) and water (50 mL), the phases were separated and the aqueous phase was extracted again with dichloromethane (50 mL). The organics were combined, dried over Na2S04 and the crude product was purified on a HP-Sil column (biotage) by employing a dichloromethane/methanol gradient (100/0 -> 90/10) to afford the title compound (83 mg, 54%). MS (ESI); m/z = 345.12 [M+H]+ 1H-NMR (400 MHz, CDCI3) d 9.53 (s, 1 H), 9.04 (d, 1 H), 8.73 (ddd, 1 H), 7.49 (dd, 1 H), 3.98 – 3.83 (m, 2H), 3.22 (s, 2H), 2.87 – 2.66 (m, 2H), 2.33 (s, 3H).

As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference£º
Patent; AC IMMUNE SA; MOLETTE, Jerome; (0 pag.)WO2019/234243; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of Example 1(d) (25ml) was treated with anhydrous potassium carbonate (1.76g) and n-heptyl iodide (2.88g) and stirred at room temperature for 18 hours.. The mixture was evaporated to dryness, treated with sodium carbonate solution, extracted with dichloromethane, dried, and chromatographed on silica gel eluding with 30-50% ethyl acetate-hexane to afford a pale yellow oil (1.5g) with ee >98% by chiral HPLC [Chirapak AD column; with hexane-ethanol (97:3)]. MS (+ve ion electrospray) m/z 315 (MH+).

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; SmithKline Beecham plc; EP1187828; (2004); B1;,
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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

General procedure: General procedure for the synthesis of 15b-15u. To a solution ofcompound 13a (0.41 g, 1.06 mmol) in 2-butanol (5 mL), 1-(2-(dimethylamino)ethyl)-1H-pyrazol-4-amine (0.196 g, 1.27 mmol)and trifluoroacetic acid (94 mL) were added in a sealed tube. Thereactionwas heated at 95 C for 18 h. The reaction mixturewas thenallowed to cool to room temperature. The mixture was transferredto a round-bottom flask and then the solvent was removed underreduced pressure. The residue was dissolved in DCM (2.0 mL) andTFA (2.0 mL), and the resulting mixture was stirred for 5 h at roomtemperature. The solvent was removed under reduced pressure,and the residue was neutralized with saturated NaHCO3 aqueoussolution. The water layer was extracted with DCM. The organiclayer was combined and washed with brine, dried over Na2SO4,filtered, concentrated, and purified by silica gel chromatography toafford 15a as a yellow solid (0.264 g, 65% for two steps).

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various.

Reference£º
Article; Yu, Lei; Huang, Minhao; Xu, Tianfeng; Tong, Linjiang; Yan, Xiao-e; Zhang, Zhang; Xu, Yong; Yun, Caihong; Xie, Hua; Ding, Ke; Lu, Xiaoyun; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 1107 – 1117;,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of 5-bromobenzofuran (250 mg, 1.27 mmol, 1.0 equiv.) and 2-methylpiperazine (508.4 mg, 5.08 mmol, 4.0 equiv.) in toluene (7 mL) was added PdCl2[P(o-Tol)3]2 (30 mg, 0.04 mmol, 0.04 equiv.) followed by sodium tert-butoxide (183 mg, 1.91 mmol, 1.5 equiv.). The resulting mixture was heated to 100 C. with stirring under nitrogen. After stirred at same temperature for 16 hours, the reaction mixture was cooled to room temperature and then diluted with ethyl acetate (100 mL). The resulting solution was washed with water, brine and then dried over Na2SO4. After removal of solvent, the crude product was purified by chromatography to give 132 mg (48% yield) of 1-Benzofuran-5-yl-3-methyl-piperazine. 1H NMR (400 MHz, CDCl3), delta (ppm): 7.56 (d, 1H), 7.39(d, 1H), 7.10 (d, 1H), 7.00 (dd, 1H), 6.69 (m, 1H), 3.44 (d, 2H), 306 (m, 3H), 2.72 (dt, 1H), 2.38 (d, 1H), 1.14 (d, 3H).

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(0104) Compound 5K (3.39 g), Compound 5A (1.87 g), 1-ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (2.39 g), and 4-dimethylaminopyridine (1.09 g) were stirred in CH2Cl2 (40 ml) for 24 hours. The reaction was cooled and chromatographed on silica gel with 25-100% ethyl acetate/hexanes, then 10% methanol/ethyl acetate with 1% acetic acid, to give the product (1.62 g, 32%) as a white solid. 1H NMR (300 MHz, dimethylsulfoxide-d6) delta 11.65 (br s, 1H), 8.55 (br s, 1H), 8.04 (d, 1H), 7.89 (dd, 1H), 7.51 (m, 3H), 7.33 (d, 2H), 7.08 (m, 1H), 7.04 (d, 2H), 6.68 (dd, 1H), 6.39 (d, 1H), 6.19 (d, 1H), 3.84 (m, 1H), 3.30 (m, 4H), 3.07 (m, 4H), 2.73(m, 2H), 2.18 (m, 6H), 1.95 (m, 2H), 1.61 (dd, 2H), 1.38 (m, 2H), 1.24 (m, 4H), 0.92 (s, 6H).

As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

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.54699-92-2,4-Methyl-1-piperazineacetic acid,as a common compound, the synthetic route is as follows.

Example 13; General Method For The Preparation Of Active Esters Of N-Substituted Piperazine Acetic Acid From Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

As the paragraph descriping shows that 54699-92-2 is playing an increasingly important role.

Reference£º
Patent; Applera Corporation.; US2005/148773; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics