Month: April 2021

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.

59878-57-8, Example 2: Alternative synthesis of Compound A using i-fcyclopropylcarbonyl) piperazineMethods (also for Examples 3 & 4)NMR1H NMR spectra were recorded using Bruker DPX 400 spectrometer at 400 MHz. Chemical shifts were reported in parts per million (ppm) on the delta scale relative to tetramethylsilane internal standard. Unless stated otherwise all samples were dissolved in DMSOd6.Mass SpectraMass spectra were recorded on an Agilent XCT ion trap mass spectrometer using tandem mass spectrometry (MS/MS) for structural confirmation. The instrument was operated in a positive ion elctrospray mode.(a) 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (Compound A)2-Fluoro-5-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]benzoic acid (D)(15.23g, 51.07 mmol) was suspended with stirring under nitrogen in acetonitrile (96 ml). Diisopropylethylamine (19.6 ml, 112.3 mmol) was added followed by 1-cyclopropylcarbonylpiperazine (l)(9.45g, 61.28 mmol) and acetonitrile (1 ml). The reaction mixture was cooled to 18C. O-Benzotriazol-1-yl- tetramethyluronium hexafluorophosphate (25.18g, 66.39 mmol) was added over 30 minutes and the reaction mixture was stirred for 2 hours at room temperature. The reaction mixture was cooled to 3C and maintained at this temperature for 1 hour, before being filtered. The filter cake was washed with cold (3C) acetonitrile (20 ml) before being dried in vacuo at up to 4O0C to give the title compound as a pale yellow solid (20.21 g).Mass Spectrum: MH+ 4351H NMR (400MHz. DMSO-d6) delta: 0.70 (m, 4H), 1.88 (br s, 1 H), 3.20 (br s, 2H), 3.56 (m, 6H), 4.31 (s, 2H), 7.17 (t, 1 H), 7.34 (dd, 1 H), 7.41 (m, 1 H), 7.77 (dt, 1 H), 7.83 (dt, 1 H), 7.92 (d, 1 H), 8.25 (dd, 1 H), 12.53 (s, 1 H).

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

Reference£º
Patent; KUDOS PHARMACEUTICALS LIMITED; WO2008/47082; (2008); 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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

EXAMPLE 24A 3-methyl-1-pyridin-2-ylpiperazine hydrobromide 2-Methylpiperazine (1.0 g, 0.01 mol, racemic mixture) and 2-bromopyridine (10 mL, 0.1 mol) were combined and heated at 120 C. for 16 hours. The reaction mixture was cooled to 23 or and partitioned between ethyl acetate and water. The layers were separated, and the water layer was concentrated under reduced pressure. The residue was triturated with ethyl acetate, dichloromethane, and methanol to afford 460 mg (26% yield) of the title compound as an off-white solid. 1H NMR (300 MHz, DMSO-d6) delta 1.27 (d, J=6.6 Hz, 3H), 2.90 (dd, J=10.5, 14.1 Hz, 1H), 3.10 (m, 2H), 3.40 (m, 2H), 4.32 (m, 2H), 6.77 (dd, J=4.8, 6.9 Hz, 1H), 6.98 (d, J=8.1 Hz, 1H), 7.64 (m, 1H), 8.15 (m, 1H), 8.63 (bs, 1H), 8.92 (bs, 1H); MS (APCI) m/e 178 (M+H)+.

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

Reference£º
Patent; Cowart, Marlon D.; Patel, Meena V.; Kolasa, Teodozyi; Brioni, Jorge D.; Rohde, Jeffrey J.; Engstrom, Kenneth M.; Stewart, Andrew O.; Daanen, Jerome F.; Bhatia, Pramila A.; US2004/127504; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8,59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a microwave vial were added methyl 4-((3-methylen-4-oxo-1,2,3,4-tetrahydrocarbazol-9-yl)methyl)benzoate [formula 2-4] (0.10 g, 0.290 mmol), 1-(cyclopropylcarbonyl)piperazine (0.134 g, 0.869 mmol) and toluene (3.0 mL), and a reaction was carried out in a microwave reactor at 120 C. for 90 minutes. Then, the reaction mixture was extracted with ethyl acetate and saturated NH4Cl aqueous solution, the organic layer was washed with brine, dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure. Residue was purified by column chromatography (SiO2; dichloromethane/methanol, 10/1) to yield the title compound (0.056 g, 39%).

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; Kim, Yuntae; Lee, Changsik; Yang, Hyun-mo; Choi, Hojin; Min, Jaeki; Kim, Soyoung; Kim, Dal-Hyun; Ha, Nina; Kim, Jung-Min; Lim, Hyojin; Ko, Eunhee; US2014/315889; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 5 1-Cyclopropyl-6,8-difluoro-1,4-dihydro-5-methyl-7-[3-methyl-1-piperazinyl]-4-oxo-3-quinolinecarboxylic acid A suspension of 0.80 g (2.69 mmol) of 1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-5-methyl-4-oxo-3-quinolinecarboxylic acid, 1.08 g (10.8 mmol) of 2-methylpiperazine, and 20 ml of acetonitrile was refluxed for three hours, then cooled in an ice bath. The precipitate was filtered, washed with water and acetonitrile, and dried to give 0.76 g of the title compound, mp 187-188 C., 109-07-9

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

Reference£º
Patent; Warner-Lambert Company; US4920120; (1990); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

A mixture of starting material (28 mg, 0.1 mmol), 2-methoxy-4-(4-methylpiperazin-1-yl)benzenamine (22 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in t-BuOH (1.5 mL) was heated at 100 C. in a seal tube for 4 h. The reaction was then filtered through celite, eluted with dichloromethane, and concentrated in vacuo. The residue was then purified by reverse-phase prep-HPLC to afford the title compound as the TFA salt (7.2 mg, 15%)., 122833-04-9

As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; Gray, Nathanael S.; Waller, David; Choi, Hwan Guen; Wang, Jinhua; Deng, Xianming; (104 pag.)US2016/24115; (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.288251-85-4,tert-Butyl 4-(4-amino-2-cyanophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Crude 4-(4-amino-2-cyano-phenyl)-piperazine-l-carboxylic acid tert-butyl ester from above was dissolved in methylene chloride (10 mL) and to the resulting solution was added 2-phenyl-5-trifluoromethyl-oxazole-4-carboxylic acid (454 mg), triethylamine(247 muL) and l-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (EDCI,337 mg). The reaction mixture was stirred at room temperature for 3 hr. Another portion of l-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (0.5 eq) was added. The reaction mixture was stirred at 500C for 3 hr and at room temperature for 3.5 days.The reaction mixture was partitioned between ethyl acetate and water. The organic layer was dried over sodium sulfate, filtered and evaporated. Purification by flash chromatography afforded 4- {2-cyano-4-[(2-phenyl-5-trifluoromethyl-oxazole-4- carbonyl)-amino]-phenyl}-piperazine-l-carboxylic acid tert-butyl ester (240 mg, 25 % yield) as a yellow solid. LCMS calcd for C27H26F3N5O4 (m/e) 541, obsd 542 (M+H)., 288251-85-4

288251-85-4 tert-Butyl 4-(4-amino-2-cyanophenyl)piperazine-1-carboxylate 22227872, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; WO2008/141976; (2008); 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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

The 100 mg compound II, 75 mg compound III by adding 5 ml dichloromethane (DCM) in, stirring, 40 C reaction 2 hours, TLC monitoring, after the reaction, the solvent turns on lathe does, the reactant putting into the 100 ml water, ethyl acetate (20 ml ¡Á 3) extraction, standing liquid, organic phase are respectively 5% of NaHCO3 (20 Ml ¡Á 3), saturated salt water (20 ml ¡Á 3) washing, then drying water-free magnesium sulfate, filtered, reduced pressure to remove the ethyl acetate to get the yellow oily compound IV 83 mg.

20327-23-5, The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Southern Medical University; Chen Jianjun; Cheng Binbin; (22 pag.)CN109456284; (2019); 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.1214196-85-6,1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a mixture of l-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (200 mg, 0.86 mmol) and DIPEA (333 mg, 2.58 mmol) in THF (8 mL) and DMF (0.5 mL) was dropped a solution of Compound 7B (216 mg, 0.86 mmol) in THF (8 mL) at 0 C. The reaction mixture was stirred at room temperature under nitrogen overnight and concentrated under reduced pressure. The residue was purified with reverse phase chromatography eluting with 25%-50% methanol in water (0.1% MLOH) to give Compound 7C: LC-MS (ESI) m/z: 445 [M+H]+., 1214196-85-6

1214196-85-6 1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid 22507584, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOMARIN PHARMACEUTICAL INC.; WANG, Bing; (270 pag.)WO2019/104011; (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.1238951-37-5,(2S,5S)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of 2,4,6-trichloro-8-fluoro-7-(2-fluoro-6- methoxyphenyl)quinazoline (2 g, 5.34 mmol) in DCM (2OmL) at 0 ¡ãC, TEA (1.08 g, 10.7 mmol) was added and then (2R,5S)-tert-butyl 2,5-dimethylpiperazine-1- carboxylatet (1.15 g, 5.34 mmol) in DCM (20 mL) was added slowly. The mixture was stirred at RT overnight. The mixture was partitioned between water (5OmL) and DCM(lOOmL X 2).The organic layer was concentrated in vacuo and the residue was purified by flash column chromatography on silica gel to afford the desired product 3-2 (2.1 g). ESI-MS m/z: 553 [M+H]., 1238951-37-5

The synthetic route of 1238951-37-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARAXES PHARMA LLC; LI, Liansheng; FENG, Jun; WU, Tao; LIU, Yuan; WANG, Yi; REN, Pingda; LIU, Yi; (110 pag.)WO2018/218069; (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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

A solution of 2-methyl-5-fluoroquinazoline (100 mg; 0.616 MMOL ; 1EQ), 2- methylpiperazine (310 mg; 3.083 MMOL ; 5eq) and triethylamine (0.17 mL; 1.23 MMOL ; 2 eq) in dry DMF (2.5 mL) was heated at 120C for 5 h. The yellow solution was cooled and the solvent was evaporated in vacuo. The crude material was purified on SPE cartridge (Si; 2 g) eluting with a gradient from 100% dichloromethane to 85% DICHLOROMETHANE : 1% NH40H 2M sol in methanol to afford the title compound (D15) (85 mg; yield 57%). MS; (ES) m/z: 243.3 [MH+]. CAHSN4 requires 242.32. ‘H NMR (300MHZ, CDCI3) 8 : 9.48 (s, 1H), 7.81 (t, 1H), 7.48 (d, 1H), 7.10 (d, 1H), 3.03 (m, 1H), 3.23-2. 98-2.76-2. 41 (m, 6H), 2.72 (s, 3H) 1.01 (d, 3H).

109-07-9, The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/46124; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics