Month: September 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.112257-12-2,tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

4-(2-bromoacetyl)piperazine-1-carboxylate (9.77 mmol, 1 eq.) in methanol (26 ml) at 0C. The reaction vial was sealed and the mixture stirred vigorously overnight at room temperature. The solvent was subsequently evaporated, the residue dissolved in hydrogen chloride (aqueous soln., 0.1 N, 100 ml) and extracted with ethyl acetate (3 x 100 ml). The pH of the recovered aqueous layer was adjusted to 10 by addition of sodium hydroxide (aqueous soln., 1 N), then the organics extracted with ethyl acetate (3 x 100 ml). The combined organic layers were dried over magnesium sulfate, filtered and the solvent evaporated under vacuum to give a light yellow crude product. Further trituration in diethyl ether conducted to the desired amine as a white solid used for the next step without additional purification. C11 H21N3O3; yield 58%; white solid; m.p. 159-160 C; M = 243.30 g/mol; IR (ATR): v = 2974 (w), 1675 (s), 1627 (s), 1417 (m), 1360 (m), 1235 (m), 1172 (m), 1123 (m), 990 (m), 759 (m) cm – ; H NMR (250 MHz, CDCI 3) delta 3.71-3.41 (m, 10H), 1.46 (s, 9H); C NMR (63 MHz, CDCI 3) delta 169.5 (C q), 154.6 (C q), 80.5 (C q), 50.4 (CH 2), 44.6 (2CH 2), 41.7 (2CH 2); HRMS: calcd. for CHH21 3O3 244.1661 , found. 244.1657;, 112257-12-2

The synthetic route of 112257-12-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTON UNIVERSITY; GRIFFIN, Martin; RATHBONE, Daniel; BADARAU, Leonas Eduard; WO2014/57266; (2014); 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.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.

4-Cyclopropylmethyl-piperazine-1-carboxylic acid 4-(4-trifluoromethyl-phenoxy)-phenyl Ester The hydrochloride of the title compound was prepared from 4-(4-trifluoromethyl-phenoxy)-phenyl chloroformate and 1-cyclopropylmethyl-piperazine, yield 43%. White crystals, m.p. 238-2390C; IR (KBr): nu 1725 (C=O) cm-1.

57184-25-5, As the paragraph descriping shows that 57184-25-5 is playing an increasingly important role.

Reference：
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Method B: Oxalyl chloride (2 M in CH2Cl2) was added dropwiseto an ice-cooled solution of 2 in dry CH2Cl2 under an argon atmosphere. After 1 h, the ice-bath was removed and the reaction batch was stirred overnight at ambient temperature in an atmosphere of Ar. Subsequently the solvent was evaporated in vacuo and the crude acyl chloride was dissolved in dry DMF and added dropwise to a stirred suspension of amine and K2CO3 in dry DMF at 0 °C. The stirring was continued for 1 h and then at ambient temperature overnight. After 20 h the suspension was filtered, the solvent evaporated, the residue taken up in water and extracted with CH2Cl2. The organic layer was washed with 5percent aqueous NaHCO3 and brine.Then it was dried over anhydrous sodium sulfate, filtered and the solvent was evaporated in vacuo yielding the raw quinoline-4-carboxamides 9?11, which were further purified by column chromatography., 934-98-5

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Hochegger, Patrick; Faist, Johanna; Seebacher, Werner; Saf, Robert; Maeser, Pascal; Kaiser, Marcel; Weis, Robert; Bioorganic and Medicinal Chemistry; vol. 25; 7; (2017); p. 2251 – 2259;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Compound 4 0.2 g (0.41 mmol) and 25 muL piperdine (0.82 mmol) was added to the 1.0 mL dried CH2Cl2.Anhydrous Na2CO3 20 mg was then added to the mixture, which was stirred for 12 h. The mixturewas washed with the distilled water, the organic phase was separated and dried over anhydrousNa2SO4, and then concentrated viarotary evaporation. The crude product was purified by silica gelchromatography with petroleum ether?acetone?strong ammonia water (v/v/v, 8/1/0.1) as the eluentto gain 0.18 g yellow solid compound 5a in 90percent yield.

4318-42-7, As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference：
Article; Feng, Xiu E.; Wang, Qin Jin; Gao, Jie; Ban, Shu Rong; Li, Qing Shan; Molecules; vol. 22; 12; (2017);,
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.1217599-13-7,(R)-1-Boc-2-Isobutylpiperazine,as a common compound, the synthetic route is as follows.

(R)-tert-but l 4-(6-chloro-5-cyano-3-fluoropyridin-2-yl)-2-isobutylpiperazine-l-carboxylateA mixture of tert-butyl (2R)-2-isobutylpiperazine-l-carboxylate (515 mg, 2.13 mmol), 2,6- dichloro-5-fluoro-pyridine-3-carbonitrile (405.9 mg, 2.13 mmol) and DIPEA (274.6 mg, 370.1 mu, 2.13 mmol) in NMP was heated at 130 C for 20 minutes under microwave conditions. After this time, the reaction mixture was allowed to cool to ambient temperature and diluted with EtOAc and water. The organic layer was separated and washed with brine, dried ( a2S04), filtered and concentrated in vacuo. The crude mixture was purified by column chromatography (ISCO Companion, 120 g column, eluting with EtO Ac/Petroleum ether) to give the sub title compound (629.9 mg, 75% Yield). XH NMR (400 MHz, CDC13) delta 7.37 (d, J= 12.6 Hz, 1H), 4.55 – 4.23 (m, 3H), 4.1 1 (q, J= 7.2 Hz, 1H), 3.23 (dd, J= 13.4, 3.6 Hz, 1H), 3.08 (d, J= 9.4 Hz, 2H), 1.64 – 1.52 (m, 1H), 1.50 – 1.28 (m, 1 1H), 0.93 (d, J= 6.5 Hz, 6H).

1217599-13-7, As the paragraph descriping shows that 1217599-13-7 is playing an increasingly important role.

Reference：
Patent; VERTEX PHARMACEUTICALS INCORPORATED; JIMENEZ, Juan-Miguel; GOLEC, Julian, M.C.; SETTIMO, Luca; FRAYSSE, Damien; BRENCHLEY, Guy; BOYALL, Dean; TWIN, Heather; YOUNG, Stephen; MILLER, Andrew, W.; DAVIS, Christopher, John; WO2011/94283; (2011); 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.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.,57184-25-5

The cis-isomer may be prepared analogously. cis- and trans-4-(4-cyclopropylmethyl-piperazin-1-yl)-cyclohexylamine 9.8 g (33.4 mmol) of 4-dibenzylcyclohexanone is dissolved in 100 mL dichloromethane and stirred with 5.6 g (40 mmol) of N-cyclopropylmethylpiperazine and 8.5 g (40 mmol) of NaBH(OAc)3 for 12 h at RT. Then the mixture is combined with water and potassium carbonate, the org. phase is separated off and dried and the solvent is eliminated in vacuo. The residue is purified on a silica gel column (approx. 50 mL silica gel, approx. 3 L ethyl acetate 95/methanol 5+0.25% conc. ammonia). The desired fractions are evaporated down in vacuo. The faster eluding cis compound crystallises from ethyl acetate. The trans compound is crystallized from ethanol+conc. HCl. Yield: 8.5 g (61%) cis-isomer and 2.2 g (13%) trans-isomer.

The synthetic route of 57184-25-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Boehringer Ingelheim International GmbH; US2006/35903; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a mixture of 5-cyclopropyl-5-phenyl- (0.01 mol; 1) or 5-cyclopropyl-5-(4-chlorophenyl)-imidazolidine-2,4-dione (0.01 mol; 2), 40% solution of formaldehyde (0.01 mol) in 96% ethanol (20 mL), corresponding 4-substituted piperazines (0.01 mol), tetrahydroisoquinoline (THIQ) or morpholine dissolved in 96% ethanol (10 mL) were added. The mixture was left for ca. 12 h at room temperature and then refrigerated at ca. -10 C for 24 h. The precipitated crude products were washed with cold ethanol, separated by filtration and recrystallized from 96% ethanol.

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Byrtus, Hanna; Obniska, Jolanta; Czopek, Anna; Kami?ski, Krzysztof; Paw?owski, MacIej; Bioorganic and Medicinal Chemistry; vol. 19; 20; (2011); p. 6149 – 6156;,
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

5-(Oxiran-2-yl)-2-benzofuran-1(3H)-one (1.5 g, 8.5 mmol) and commercially ayailable (S)-4-N-BOC-2-hydroxymethyl piperazine (2.394 g, 11.07 mmol) were combined in ethanol (10 mL) in a microwaye tube. The mixture was degassed then heatedfor 60 min at 150 C. Lc-MS showed the product peak. The reaction was worked up by adding ethyl acetate and washing once with brine. The organie layer was separated, dried, and concentrated to dryness. The crude product was purified by MPLC using an 80g Redi-sep column and eluted with 50%-100% EtOAc/ hexane yielding 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; DE JESUS, Reynalda, Keh; DING, Fa-xiang; DONG, Shuzhi; FRIE, Jessica; GU, Xin; JIANG, Jinlong; SHAHRIPOUR, Aurash; PIO, Barbara; TANG, Haifeng; WALSH, Shawn; WO2014/126944; (2014); 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.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

Example 280 6-(2,3-dimethylphenyl)-4-N-{[4-(4-m 2,4-diamine. A mixture of 4-chloro-6-(2,3-dimethylphenyl)pyrimidin-2-amine (23 mg, 0.10 mmol), [4-(4-methylpiperazin-1-yl)phenyl]methanamine (29 mg, 0.14 mmol) and Hunig’s base (35 muIota_, 0.20 mmol) in n-butanol (1.5 ml_) was heated in a sealed tube at 85C overnight. The reaction mixture was concentrated and purified by preparative HPLC. LCMS [M+H]+ 403.

216144-45-5, 216144-45-5 4-(4-Methylpiperazin-1-yl)benzylamine 2776493, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; THOMAS HELLEDAYS STIFTELSE FOeR MEDICINSK FORSKNING; SCOBIE, Martin; WALLNER, Olov; KOOLMEISTER, Tobias; VALLIN, Karl Sven Axel; HENRIKSSON, Carl Martin; HOMAN, Evert; HELLEDAY, Thomas; JACQUES, Sylvain; DESROSES, Matthieu; JACQUES-CORDONNIER, Marie-Caroline; FISKESUND, Roland Julius Yu; (359 pag.)WO2015/187089; (2015); 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

Ethyl 5-chloro-l ,3,4-thiadiazole-2 -carboxylate (3, 3 g, 15.7 mmol), 2-methoxy-4-(4-methyl piperazin-l -yl)aniline (4, 3.4 g, 15.7 mmol) and p-TSA (3 g, 15.7 mmol) were taken up in IPA (25 mL) and the resultant mixture was stirred at 80 C overnight. The progress of the reaction was monitored by TLC. After completion of the reaction, the solvent was evaporated from the reaction mixture under reduced pressure, and the resultant residue was basified using aq. NaHC03 solution and extracted with ethyl acetate. The organic extract was dried over anhydrous sodium sulfate and evaporated under reduced pressure. The resultant crude product was purified by columnchromatography using 5% MeOH-DCM to afford ethyl 5-((2-methoxy-4-(4-methylpiperazin-l – yl)phenyl)amino)-l ,3,4-thiadiazole-2-carboxylate (5, 1 .5 g, 25%). NMR (400 MHz, CDC13): delta 7.90 (bs, 1 H), 7.43 (d, 1 H), 6.59-6.55 (m, 2H), 4.50 (q, 2H), 3.90 (s, 3H), 3.25-3.22 (m, 4H), 2.65- l .60 (m, 4H), 2.40 (s, 3H), 1.42 (t, 3H)., 122833-04-9

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

Reference：
Patent; GATEKEEPER PHARMACEUTICAL, INC.; GRAY, Nathanael, S.; ZHOU, Wenjun; WO2011/79231; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics