Tag: M.W:200-300

438631-77-7, (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 7-bromo-4,6-dichloro-3-nitroquinoline (4.97 g, 15.44 mmol) in THF (100 mL) was added 1-tert-butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (4.9 g, 20.07 mmol) followed by DIPEA (8.07 mL, 46.31 mmol) and reaction mixture heated at reflux overnight. Further 1-tert-butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (0.943 g, 0.25 eq) was added, along with further DIPEA (1.35 mL, 0.5 eq) and the reaction mixture heated at reflux for a further 24 h. The reaction mixture was partially concentrated and partitioned between water and EtOAc. Layers were separated, the organic layer washed with water and the combined aqueous layers were back extracted with EtOAc. The combined organic layers were dried (phase separator) and concentrated in vacuo to afford crude material as a dark brown oil. This was purified by flash silica chromatography (0 to 18% EtOAc in heptane) to afford 1-tert-butyl 3-methyl (3R)-4-(7-bromo-6-chloro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (5.2 g, 64%) as an orange foam; 1H NMR (400 MHz, DMSO, 30 C.) 1.44 (9H, s), 3.29 (2H, s), 3.5-3.58 (3H, m), 3.6-3.69 (1H, m), 3.73 (1H, dd), 3.78-3.9 (1H, m), 4.02-4.2 (1H, m), 4.3-4.38 (1H, m), 8.49 (1H, s), 8.52 (1H, s), 9.11 (1H, s); m/z: ES+ [M+H]+ 529, 531.

438631-77-7, The synthetic route of 438631-77-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

697305-48-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.697305-48-9,1-(4-Fluorophenyl)piperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

General procedure: To a suspension of ethyl (2R,3S)-2-amino-3-(1H-indol-3-yl)butanoate methanesulfonate 4 (606 mg, 1.8 mmol) and CDI (476 mg, 2.9 mmol) in MeCN (10 mL) was added dropwise DIEPA (0.67 mL) and stirred at 0 C for 30 min. 8a (410 mg, 1.8 mmol) and DIPEA (0.35 mL) was added to the mixture, and stirred ar room temperature overnight. The mixture was added sat. NaHCO3 aq., and extracted with AcOEt. The organic layer was washed with brine, dried over MgSO4, and concentrated in vacuo. The residue was purified by column chromatography to give 6a as a amorphous solid. The obtained material was dissolved in EtOH (5 mL) and was added dropwise 4 N NaOH (1.4 mL). The resulting mixture was stirred room temperature overnight. After evaporation of the solvent, the residue was acidified with 1 N HCl and the resulting precipitate was collected by filtration, washed with H2O to give 7a (630 mg, 81%) as a colorless solid.

697305-48-9 1-(4-Fluorophenyl)piperazin-2-one hydrochloride 67085022, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Banno, Yoshihiro; Sasaki, Shigekazu; Kamata, Makoto; Kunitomo, Jun; Miyamoto, Yasufumi; Abe, Hidenori; Taya, Naohiro; Oi, Satoru; Watanabe, Masanori; Urushibara, Tomoko; Hazama, Masatoshi; Niwa, Shin-ichi; Miyamoto, Saku; Horinouchi, Akira; Kuroshima, Ken-ichi; Amano, Nobuyuki; Matsumoto, Shin-ichi; Matsunaga, Shinichiro; Bioorganic and Medicinal Chemistry; vol. 25; 21; (2017); p. 5995 – 6006;,
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.373608-48-1,tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of intermediate compound E1 (1 .1 g), triethylamine (0.674 ml_) and 2-oxo-2H-chromen-4-yl trifluoromethanesulfonate (1 .2 g), prepared as described in step 5 of the preparation of compound 51 , in acetonitrile (20 ml_) was heated to 705C for 1 hour. The reaction mixture was concentrated under reduced pressure and the residue was partitioned between dichloromethane and a brine/sodium bicarbonate mixture (1 :1 ). The mixture was filtered through a hydrophobic frit (Phase Separator) washing with dichloromethane. The organic phase was evaporated under reduced pressure and the residue was chromatographed on silica gel (SNAP50) eluting with a gradient of EtOAc in cyclohexane to give 700 mg of tert-butyl 4-{3-[(2-oxo-2H-chromen- 4-yl)amino]propyl}piperazine-1 -carboxylate intermediate compound E2 (700 mg, Y=44%). LC-MS (M-H+) = 388.3, 373608-48-1

As the paragraph descriping shows that 373608-48-1 is playing an increasingly important role.

Reference：
Patent; AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.; OMBRATO, Rosella; GAROFALO, Barbara; MANGANO, Giorgina; CAPEZZONE DE JOANNON, Alessandra; CORSO, Gaia; CAVARISCHIA, Claudia; FURLOTTI, Guido; IACOANGELI, Tommaso; (161 pag.)WO2016/96686; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

11 g (2.35 g, 10 mmol) was dissolved in a methanol solvent,Under nitrogen protection, 200 mg of Pd / C was added,And then through the H2 reaction,6h after the reaction is complete.The filtrate was collected by filtration, and concentrated to give 1.89 g of a solid. Yield 92%., 70261-81-3

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Nantong University; Ling, Yong; Mou, Jiefei; Xu, Qibing; Feng, Jiao; Zhu, Peng; Liu, Ji; Wang, Tingting; Ge, Xiang; Liang, Shanshan; (26 pag.)CN106432235; (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.438631-77-7,(R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.,438631-77-7

To (R)-1-tert-butyl 3-methylpiperazine-1,3-dicarboxylate (1.2 g, 4.9 mmol, ASW Med Chem Inc) in MeCN and MeOH (1:1, 100 mL) was added formaldehyde (37% aqueous, 13.2 mL, 177 mmol), followed by the addition of sodium triacetoxyborohydride (5.20 g, 24.5 mmol). The mixture was stirred for about 15 min at ambient temperature. AcOH (5.6 mL, 98 mmol) was added drop-wise and the mixture was stirred for about 1 h. The solvent was removed under reduced pressure and the residue was dissolved in DCM (100 mL) and neutralized using aqueous 2 N NaOH. Saturated aqueous NaHCO3 (50 mL) was added and the layers were separated. The organic layer was washed with brine (50 mL), dried over anhydrous MgSO4, filtered, and concentrated under reduced pressure. The crude material was purified by silica gel chromatography eluting with a gradient of 20-80% EtOAc/heptane to afford (R)-1-tert-butyl 3-methyl 4-methylpiperazine-1,3-dicarboxylate (1.1 g, 85%): LC/MS (Table 2, Method a) Rt=1.91 min; MS m/z: 259 (M+H)+.

438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ABBOTT LABORATORIES; US2009/312338; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-methoxy-4-(4-methylpiperazin-l-yl)aniline (331 mg, 1.5 mmol, 1 eq.) and 8-bromo-2-chloroquinazoline (363 mg, 1.5 mmol, 1 eq.) in n-BuOH (10 mL) was added TFA (0.14 mL, 1.8 mmol, 1.2 eq.). The mixture was stirred at 110 C for 12 h. The solution was then cooled to r.t. and concentrated. The resulting residue was dissolved in EA (20 mL), washed with aqueous Na2C03 solution, dried over anhydrous Na2S04and concentrated. The resulting residue was purified via column chromatography (EA/MeOH=5 : 1 , v/v) to afford 8-bromo-N-(2-methoxy-4-(4-methylpiperazin-l-yl)phenyl)quinazolin-2-amine (140 mg, 22% yield)., 122833-04-9

The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NEUPHARMA, INC.; QIAN, Xiangping; ZHU, Yong-Liang; WO2015/27222; (2015); 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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

General Procedure 3-1 : Synthesis of (4-((4-methylpiperazin-l-yl)methyl)aniline)[00187] The synthesis of the title compound was conducted as described in U.S. Pat. Appl. Publ.No. 2006058341 (March 16, 2006). Specifically, to a solution of 4-nitrobenzyl chloride in THF at the room temperature was added 1 -methyl piperazine. The solution was stirred for 3 hours after which time the crude reaction was diluted with ethyl acetate and washed repeatedly with water. The dried organics were concentrated to give directly the 4-nitrobenzylamine adduct.This was subsequently treated with Rainey Nickel in THF at 75PSI for 12 hours to give the title compound., 70261-81-3

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BIOGEN IDEC MA INC.; WO2008/94575; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

216144-45-5, 4-(4-Methylpiperazin-1-yl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1-chloro-4-methoxy-5-nitro-2-vinylbenzene (0.42 g,1.95 mmol), 4-(4- methyl-piperazin-1-yl)-benzylamine (1.2 g, 5.85 mmol) and quinol (0.043 g, 0.39 mmol) in n-butanol (8 mL) was heated to reflux for 12 hours under a N2 atmosphere. Water (100 mL) was added and the reaction mixture extracted with EtOAc (3 X 100 mL). The combined organic extracts were washed with brine (50 mL), dried (Na2S04) and concentrated under reduced pressure. The residue was purified by columnchromatography on neutral silica gel using 3-5% methanol in DC to give the title compound (0.35 g, 43%) as a solid.

216144-45-5, As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference：
Patent; SENTINEL ONCOLOGY LIMITED; BOYLE, Robert George; WALKER, David Winter; BOYCE, Richard Justin; WO2011/141716; (2011); 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.

Step C: tert-butyl (38)-4-[2-(2, 1 ,3-benzoxadiazol-5-yl)-2-hydroxyethyll -3-(hydroxymethyl)piperazine-1-carboxylate: To a microwave tube containing a stir bar was added5-(oxiran-2-yl)-2,1,3-benzoxadiazole (1.2 g, 7.4 mmol), Boc-piperizine alcohol (2.8 g, 13.3mmol); the resulting mixture was dissolved in anhydrous toluene (15 mL), purged with N2 andthe tube was heated in a microwave reactor for 1 h at 150 C. TLC analysis of the rectrion mix.showed the completion of the reaction. The solution was concentrated to dryness and absorbed into silica gel and was subjected for purification over a silica column to give 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：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To an aqueous (100 ml) sodium hydroxide (4.0 g, 100 mmol) solution of piperazine-2-carboxylic acid dihydrochloride (5 g, 24.63 mmol) is added a solution of di-tert-butyl dicarbonate (11.0 g, 50.45 mmol) in dioxan (50 ml) at 0 C. over a period of half an hour. The reaction mixture is stirred at 0 C. for 1 hr. followed by stirring at room temperature (25 C.) for another 2 hrs. Neutralized (pH 6-7) with aqueous 2N HCl, extracted with ethyl acetate. Organic layer washed with brine solution, dried (Na2SO4) and evaporated in vacuo to yield an oil which solidifies on cooling. (Yield 8.02 g, 98.76%)., 3022-15-9

The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TORRENT PHARMACEUTICALS LTD.; US2003/225102; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics