Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.34334-28-6,4-(4-Methylpiperazin-1-yl)benzonitrile,as a common compound, the synthetic route is as follows.

To a solution of 13 (1eq.) and CoCl2 6H20(2.1 eq.), NaBH4 (10 eq.) was added. The reaction mixture wasstirred for 5h and then filtered on a celite pad. The organic phase wasevaporated under reduced pressure. The yellow oil was purified by flashchromatography on silica gel (CH2Cl2:MeOH 8:2). Thedesired compound was obtained as a white solid (50%). 1H NMR (400MHz, MeOD): delta(ppm) 2.42(s, 3H); 2.74(t, J=8, 4H); 3.17(t, J=8, 4H), 4.43(s,2H); 6.89(d, J=8, 2H); 7.18(d, J=8, 2H). Anal. Calcd. for C12H19N3:C, 70.20; H, 9.33; N, 20.47; found; C, 70.10; H, 9.13; N, 20.27, 34334-28-6

34334-28-6 4-(4-Methylpiperazin-1-yl)benzonitrile 763205, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Radi, Marco; Bernardo, Vincenzo; Vignaroli, Giulia; Brai, Annalaura; Biava, Mariangela; Schenone, Silvia; Botta, Maurizio; Tetrahedron Letters; vol. 54; 38; (2013); p. 5204 – 5206;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5747-48-8

Example 3: l-(4-Dibenzo[b,f] [l,4]thiazepin-ll-yl-piperazin-l-yl)-ethanoneA solution of PDBTZ (1 mmol) (lmmol) in DMF (2 mL) is treated with acetic anhydride (2 mmol) and heated for one hour. The reaction mixture is evaporated to dryness, made basic with aqueous potassium carbonate, and extracted with dichloromethane. The organic portion is washed (water, brine), dried (sodium sulfate), and evaporated. The crude material is purified by flash chromatography to provide the title compound.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; WO2008/79838; (2008); 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

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

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.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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

Step A1, 1-dimethylethyl 4-(2-fIuoro-4-methylphenyl)-3-oxo-1-piporazinecarboxylate A mixture of 1 ,1-dimethylethyl 3-oxo-1 -piperazinecarboxylate (0.326 g, 0.00163 mol), 1-bromo-2-fluoro-4-methylbenzene (0.308 g, 0.0163 mol), (1 R,2R)-N,N’-dimethyl~ 1 ,2-cyclohexanediamine (0.026 mL, 0.163 mmol), copper(l) iodide (3.10 mg, 0.016 mmol) and potassium carbonate (450 mg, 3.26 mmol) in 1 ,4-dioxane (6 mL) in a septum-sealed vial was heated in an oil bath at 120 C overnight. The reaction mixture was cooled to room temperature and filtered through Celite washing with ethyl acetate. The filtrate was washed with saturated aqueous ammonium chloride, water and brine, dried over sodium sulfate and concentrated. The residue was purified by chromatography on silica gel to give the title compound (0. 253 g, 50%). MS (ESI) m/z: 309 (M+1 )., 76003-29-7

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; MAYNARD, Andy; MILLER, John; PATTERSON, Dan; PEAT, Andrew, James; POWERS, Jeremiah; PRICE, Daniel, J.; ROBERTS, Chris; TAI, Vincent; YOUNGMAN, Michael; WO2011/50284; (2011); A1;,
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

[0384] To a solution of l-Boc-4-(2-chloroethyl)piperazine (6.85 g, 27.62 mmol) in methanol (50 ml) was added thiourea (4.12 g, 55.24 mmol). The mixture was heated to reflux for 2 hours. A solution of sodium hydroxide (1.66 g, 41.43 mmol) in water (10 ml) was added, and the mixture was continued to reflux for another hour. Then most solvent was evaporated under reduced pressure. The residue was mixed with ethyl acetate (50 ml) and brine (30 ml) and separated. The ethyl acetate was dried over magnesium sulfate and evaporated under reduced pressure. The residue was dissolved in methanol (20 ml). 4 M hydrochloric acid in dioxane (10 ml) was added. The mixture was stirred at room temperature overnight and most of solvent was evaporated under reduced pressure. The residue was used for the addition reaction without further purification.

208167-83-3, The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SU, Zhuang; LONG, Zhengyu; YANG, Suizhou; WO2014/145686; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169448-87-7, (R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 6-bromo-4-(bromomethyl)-2-(phenylsulfonyl)isoquinolin-1 (2H)-one (Examplei 1d, 1.75 g) in THF (20 mL) was treated with (f?)-tert-butyl ethyl(1-hydroxy-3- (methylamino)propan-2-yl)carbamate (0.98 g) and /V,Lambda/-diisopropylethylamine (0.80 mL) under nitrogen. The resulting solution was stirred at 50 C for 1 h. The reaction mixture20 was diluted with water (300 mL), and extracted with ethyl acetate (250 mL x 2). The combined organics were dried (MgSO4), filtered and evaporated. Triturated with diethyl ether / isohexane (1 :1) afforded the subtitle compound (2.30 g) as a solid. 1H NMR delta (CDCI3) 8.16 – 8.10 (m, 3H), 8.06 (s, 1H), 7.90 (s, 1H), 7.71 – 7.65 (m, 1H), 7.60 – 7.54 (m, 3H), 4.23 – 4.16 (m, 1 H), 3.84 (d, 2H), 3.59 – 3.45 (m, 2H), 3.21 – 3.02 (m, 2H),2S 2.89 – 2.79 (m, 1 H), 2.33 – 2.09 (m, 3H), 1.51 (s, 9H)

169448-87-7, 169448-87-7 (R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate 24820219, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; BROUGH, Stephen, John; LUKER, Timothy, Jon; ROBERTS, Bryan, Glyn; ST-GALLAY, Stephen, Anthony; WO2010/39079; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3-4-3 Preparation of 2-[3-fluoro-4-(BOC-piperazino)]phenylamino-6-chloro-3-nitropyridine To 100ml of methanol were added 2.75g (14.2mmol) of 2,6-dichloronitropyridine and 2.38ml (17.0mmol) of triethylamine and 4.2g (14.2mmol) of [3-fluoro-4-(BOC-piperazino)]aniline obtained in Preparation Example 3-4-2 was then added thereto, followed by reaction at room temperature (20 to 30C) for about 24 hours. After the reaction was complete, the reactant was filtered, washed with 20ml of methanol and then dried under vacuum at about 40C to afford 4.47g (yield: 70%) of the desired compound. Mass (M+): 452.0 1H-NMR (DMSO-d6): 1.42(s, 9H), 2.96(t, 4H), 3.48(m, 4H), 7.01(d, 1H), 7.07(t, 1H), 7.34(d, 1H), 7.53(d, 1H), 8.53(d, 1H), 10.08(s, 1H)., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Dong Wha Pharm. Co., Ltd.; EP2394993; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics