Month: January 2021

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: 2-(4-Cyclopentyl-piperazin-1-yl)-pyrimidin-4-ylamine (Intermediate 1) A mixture of 0.5 g (3.86 mmol) 2-chloro-4-pyrimidinylamine (commercially available) and 1-cyclopentyl-piperazine (commercially available) in 1 mL DMF was heated to 70 C. for 16 h. The residue after filtration washed with diethyl ether and dried to yield 0.49 g (51%) of the title compound (intermediate 1) as white solid. MS (m/e): 284.3 (MH+)., 21043-40-3

The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nettekoven, Matthias Heinrich; Roche, Olivier; US2007/281921; (2007); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Into a 25-mL sealed tube purged and maintained under an inert atmosphere of nitrogen, was placed a solution of 6-methoxy-2-[4-[3-(piperidin-4-yloxy)azetidin-l-yl]phenyl]-l,3-benzothiazole (110 mg, 0.28 mmol, 1 equiv), K2CO3(115 mg, 0.83 mmol, 3 equiv), ter/-butyl-4-(2- chloroethyl)piperazine-l-carboxylate (69 mg, 0.28 mmol, 1 equiv), and Nal (4.2 mg, 0.03 mmol, 0.1 equiv) in CH3CN (5 mL). The resulting mixture was stirred for 16 hours at 40 C. The solids were filtered off, and the filtrate was concentrated. The residue was applied onto a silica gel column eluting with dichloromethane/methanol (10:1). This resulted in 178 mg of tert-butyl-4-[2-[4-([l-[4-(6-methoxy-l,3- benzothiazol-2-yl)phenyl] azetidin-3 -yl] oxy)piperidin- 1 -yl] ethyl Ipiperazine- 1 -carboxylate as a yellow- green solid.

208167-83-3, As the paragraph descriping shows that 208167-83-3 is playing an increasingly important role.

Reference£º
Patent; ARVINAS OPERATIONS, INC.; CREW, Andrew P; DONG, Hanqing; BERLIN, Michael; SPARKS, Steven M.; (513 pag.)WO2020/41331; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Diisopropylethylamine (156 mL, 894 mmol)was added to a stirred, room temperature mixture of 3-(2-Bromo-acetyl)-6-fluoro-2-methyl- benzonitrile (176 g, 688 mmol) and (R)-4-N-Boc-2-hydroxymethyl-piperazine (149 g, 688 mmol) in THF (3500 mL) and the mixture was stirred at room temperature for 18 h. The reaction was diluted with 3 L EtOAc, washed 2x with 1500 m 10% w/w NaHcO3 aqueous solution, driedoyer MgSO4, filtered and concentrated. The residue was purified by column chromatography on silica gel (40-80% EtOAc/Hexanes, linear gradient), to proyide the title compound.

278788-66-2, The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,74879-18-8

Triethylamine (4.13 g, 3 niL, 40.8 mmol, 4 eq) is added to a solution of 6-chloro- nicotinonitrile (1.38 g, 10 mmol, leq), (S)-2-methyl- piperazine (1.0Og, 10 mmol, leq) in DMF (15 niL), and the resulting solution is stirred at rt for 14 h. A white precipitate of triethylamine hydrochloride forms in the course of the reaction. Water (15 mL) and EtOAc (100 mL) are added, the organic layer is separated, dried over sodium sulfate and concentrated under reduced pressure to a white residue. The solid is further dried under high vacuum to yield the desired product as a white solid (1.4 g, 69%). 1H NMR (400 MHz, CHLOROFORM-cf) delta ppm 8.38 (s, 1 H), 7.58 (d, J=9.60 Hz, 1 H), 6.59 (d, J=9.09 Hz, 1 H), 4.19 – 4.31 (m, 2 H), 3.08 – 3.15 (m, 1 H), 2.92 – 3.04 (m, 1 H), 2.81 – 2.91 (m, 2 H), 2.57 – 2.65 (m, 1 H), 1.15 (d. J=6.32 Hz, 3 H).

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; WO2008/110611; (2008); A1;,
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171504-98-6, Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add 1,4-di-tert-butyl 2-methylpiperazine-1,2,4-tricarboxylate (10 g) to the dry reaction flask.29.04mmol),Anhydrous tetrahydrofuran (100 mL),Under nitrogen protection, cool down to -78 C,Slowly add LiHDMS (35 mL, 35 mmol, 1 mol/L).After stirring for 2 h, iodomethane (3.7 mL, 59 mmol) was added.Stirring was continued for 1 h, slowly warmed to room temperature, and stirring was continued for 12 h.The reaction was quenched by adding a saturated aqueous solution of ammonium chloride (50 mL), and then ethyl acetate(100 mL ¡Á 2), the organic layer was combined, and the organic layer was evaporated. ),The title compound was obtained as a colorless oil (8.2 g, 79%)

171504-98-6, As the paragraph descriping shows that 171504-98-6 is playing an increasingly important role.

Reference£º
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Liu Xinchang; Ren Qingyun; Yan Guanghua; S ¡¤geerdeman; Zhang Yingjun; (200 pag.)CN109678859; (2019); A;,
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Piperazines – an overview | ScienceDirect Topics

13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a mixture of 1-benzoylpiperazine (1.0 eq) and potassium carbonate (2.0 eq) in dimethylformamide was added dropwise a solution of the corresponding substituted 9-bromo-9H-fluorene (1.0 eq) in dimethylformamide (The synthesis of 9-bromo-9H-fluorene derivatives is reported in supporting information). After stirring for 24 h at room temperature, solvent was removed and the crude residue was dissolved in diethyl ether, washed with brine, dried over magnesium sulfate,filtered and concentrated under vacuum. The residue was purified by flash chromatography as indicated in each case to afford the title compound. Reagents: 1-Benzoylpiperazine (0.21 mmol, 40 mg), potassium carbonate (0.42 mmol, 58 mg) and 9-bromo-3-hexyloxy-9H-fluorene (0.21 mmol, 63 mg). The crude product was purified by flash chromatography (gradient, 100% petroleum ether to 100% ethyl acetate in 15 min) to afford a brown oil (54 mg, 57%). TLC Rf: 0.20 (petroleum ether/ethyl acetate 70/30). IR (cm-1): 615, 633, 670, 708, 734, 768, 788, 847, 1000, 1016, 1142, 1190, 1256, 1277, 1301, 1426, 1449, 1490, 1578, 1630, 2857, 2929. HPLC: method 2, rt = 5.36 min, purity 98%. 1H NMR (300 MHz, CDCl3) delta (ppm): 0.91-1.02 (m, 3H); 1.33-1.47 (m, 4H); 1.47-1.61 (m, 2H); 1.87 (quin, J = 6.9 Hz, 2H); 2.44 (s, 2H); 2.86 (s, 2H); 3.37 (s, 2H); 3.82 (s, 2H); 4.07 (t, J = 6.6 Hz, 2H); 4.85 (s, 1H); 6.87 (dd, J = 2.4 Hz, 8.4 Hz, 1H); 7.24 (d, J = 2.4 Hz, 1H); 7.32 (td, J = 1.5 Hz, 7.5 Hz, 1H); 7.36-7.45 (m, 6H); 7.52 (d, J = 8.4 Hz, 1H); 7.63 (d, J = 5.2 Hz, 1H); 7.67 (d, J = 6.9 Hz, 1H). 13C NMR (75 MHz, CDCl3) delta (ppm): 14.1 (CH3); 22.7 (CH2); 25.8 (CH2); 29.4 (CH2); 31.7 (CH2); 42.9 (CH2); 48.5 (CH2); 48.6 (CH2); 49.5 (CH2); 68.3 (CH2); 69.4 (CH); 105.8 (CH); 113.6 (CH); 119.7 (CH); 125.8 (CH); 126.6 (CH); 127.1 (2 * CH); 127.2 (CH); 128.2 (CH); 128.4 (2 * CH); 129.6 (CH); 135.2 (C); 135.9 (C); 141.0 (C); 142.5 (C); 144.4 (C); 159.9 (C); 170.3 (C). MS (DCI/CH4) m/z: 454.26 [M], 265.16 [M-189]. HRMS (DCI/CH4): for C30H34N2O2 [M]: calcd: 454.2620; found: 454.2607.

13754-38-6, 13754-38-6 1-Benzoylpiperazine 762654, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Chollet, Aurelien; Mori, Giorgia; Menendez, Christophe; Rodriguez, Frederic; Fabing, Isabelle; Pasca, Maria Rosalia; Madacki, Jan; Kordulakova, Jana; Constant, Patricia; Quemard, Annaik; Bernardes-Genisson, Vania; Lherbet, Christian; Baltas, Michel; European Journal of Medicinal Chemistry; vol. 101; (2015); p. 218 – 235;,
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.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

115761-79-0, Example 8 N7- {2-[4-(2,4-Difluoro-phenyl)-piperazin-1-yl]-ethyl}-2-furan-2-yl- [1, 2, 4] triazolo [1, 5-C] PYRIMIDINE-5, 7-DIAMINE 7-CHLORO-2-FURAN-2-YL- [1, 2, 4] TRIAZOLO [1, 5-c] PYRIMIDIN-5-YLAMINE (1 g; see Example 1 (b) above) was suspended in 20 mL OF DMSO along with 1.5 eq of CsF and 5 eq of aminoacetaldyde dimethyl acetal. The reaction mixture was stirred at 110 oC for 18 hours. It was then cooled to room temperature and diluted with EtOAc and washed with H20 and brine, dried with NA2S04 and concentrated to afford N7-(2, 2- dimethoxy-ethyl)-2-furan-2-yl- [1, 2,4] triazolo [1, 5-c] pyrimidine-5, 7-diamine. This dimethyl acetal intermediate (40 mg, 0.13 mmol) was then unmasked to the corresponding aldehyde by suspending in a solution of 2 mL OF CH2C12 and 0.2 mL of 2: 1 solution OF TFA/H20. The resulting reaction mixture was stirred at room temperature for 4 hours. It was then neutralized with 0.25 mL of ET3N. 1- (2, 4- Difluoro-phenyl) -piperazine (40 mg, 1.5 eq; see Example 6 (a) above) was added, followed by 140 mg of Na(OAc)3BH The resulting reaction mixture was stirred at room temperature for 2 hours. It was then concentrated and then purified by preparative HPLC to afford the title compound. 1H NMR (DMSO-d6) 8 7.60 (d, J = 1. 0 Hz, 1 H), 7.28 (br s, 2 H), 7.22 (d, J = 3.6 Hz, 1 H), 6.8-7. 3 (m, 3 H), 6.68 (dd, J = 3.6 Hz, 1.0 Hz, 1 H), 6.5 (s, 1H), 3.1 (br s, 2 H), 2.2-3. 6 (m, 12 H). MS: m/z: 441 [M + NU.

As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference£º
Patent; BIOGEN IDEC MA INC.; WO2004/92172; (2004); 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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

The preparation method of 4-hydroxyethylpiperazine ethanesulfonic acid includes the following steps: 1) Mix 260g (2mol) 2-hydroxyethylpiperazine, 165g (0.94mol) sodium 2-chloroethylsulfonate with 120mL water, stir well, the reaction solution becomes clear, the pH is about 10,Heat up to 85 , stop heating until the system self-heats to 103-105 ,The reaction is heated to reflux for 30min, the reaction is over, and the pH is about 8;2) Cool the reaction liquid to 60 C, add triethylamine to the reaction liquid to adjust the pH to 7-8, 1.5 L of absolute ethanol and 8 g of activated carbon, boil for 30 min, and filter while hot;3) Adjust the pH of the filtrate to 5 using glacial acetic acid, stir the filtrate and cool to 5 C to crystallize overnight,Filter and dry to obtain 310g of crude product, which is 95% by drying after titration inspection; 4) Dissolve the sample obtained in step 3) in 750 mL of ethanol and heat to reflux, Add 145mL of water, stir to dissolve, filter while hot, and the filtrate is cooled to 5 overnight, Filtration gave 181g of 4-hydroxyethylpiperazineethanesulfonic acid crystals, After drying, 175g of 4-hydroxyethylpiperazineethanesulfonic acid was obtained, and the content was 99.8% after titration; 5) Concentrate the mother liquor under reduced pressure to a volume of 30-40%, add activated carbon to boil for decolorization, filter while hot, the filtrate is cooled to 0-5 C, filtered, dried and recovered to obtain 15g of 4-hydroxyethylpiperazineethanesulfonic acid After titration, the content was 99.6%, and the total yield was 84.7%., 103-76-4

As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference£º
Patent; Suzhou Yake Technology Co., Ltd.; Yuan Yongkun; (10 pag.)CN110683995; (2020); 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.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A stirred solution of (3S,5R)-tert-butyl 3,5- dimethylpiperazine-1 -carboxylate (20 g, 93.0 mmol, 1 eq) in LiHMDS (200 mL) was cooled to 0C and 2,6-difluoropyridine (26.8 mL, 280.3 mmol, 3 eq), and xanthophos (3.24 g, 5 mmol, 0.06 eq) were added followed by Pd2(dba)3 (2.5 g, 2.7 mmol, 0.03 eq). Then, the resultant reaction mixture was stirred overnight at 80C. The reaction was monitored with TLC, and TLC indicated formation of a non-polar spot. The reaction mixture was quenched with ice water (100 mL), filtered through celite and washed with ethyl acetate. The layers were separated, and the aqueous layer extracted with ethyl acetate (2×150 mL) and washed with brine solution (1×100 mL). The combined organic layer was dried over Na2S04, and concentrated under reduced pressure to give crude product. The crude product was purified by column chromatography (silica gel, 100-200 mesh) using 0-5% ethyl acetate in petroleum ether as an eluent to afford (3R,5S)-tert-butyl 4-(6-fluoropyridin-2-yl)-3,5-dimethylpiperazine-1 -carboxylate (20 g, 37.73% yield) as a brown liquid. LCMS: m/z 310.54 (M+H).

129779-30-2, The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ISAAC, Methvin; CHAU, Anh My; MAMAI, Ahmed; WATSON, Iain; PODA, Gennady; SUBRAMANIAN, Pandiaraju; WILSON, Brian; UEHLING, David; (191 pag.)WO2019/119145; (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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

A mixture of Example 18B (0.179 g, 1.0 mmol), l-methylpiperazin-2-one, hydrochloric acid (0.301 g, 2 mmol), and triethylamine (0.405 g. 4.0 mmol) in ethanol (10 mL) was heated under reflux for 16 hours. The solvent was removed, and the residue was purified by flash column chromatography on silica gel eluting with 1-5 % methanol in ethyl acetate to afford 0.21 g (82%) of the title compound.

109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ABBOTT LABORATORIES; ABBOTT LABORATORIES TRADING (SHANGHAI)COMPANY, LTD.; HUBBARD, Robert Dale; MCDANIEL, Keith F.; PARK, Chang Hoon; PRATT, John K.; SOLTWEDEL, Todd; SUN, Chaohong; WANG, Le; WENDT, Michael D; WO2013/185284; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics