Tag: 169447-70-5

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Intermediate 6: 4-{[(3S)-3-Meth l-1 -piperazinyl]sulfonyl}benzonitrileTo a solution of 1 ,1 -dimethylethyl (2S)-2-methyl-1 -piperazinecarboxylate (2.5g, supplier Atlantic Scitech) and DIPEA (5.45 ml, 31 .2 mmol) in dry dichloromethane (DCM) (60 ml) at 0C under argon was added 4-cyanobenzenesulfonyl chloride (2.64 g, 13.1 1 mmol) and the resulting clear solution stirred at 0C for 2h. Saturated aqueous NaHC03 (100 mL) was added, the layers separated, then the organic layers washed with 2M aqueous HCI (100 mL) and passed through a hydrophobic frit. The solution in DCM was cooled to 0C, then TFA (8.87 ml, 1 15 mmol) was added. The resulting very pale yellow solution was allowed to warm to room temperature over 1 h, then stirred for 18h. Aqueous 2M NaOH (100 mL) was added cautiously with cooling (0C) and layers were separated. The organic layer was extracted with 1 M aqueous HCI (3X30 mL). With cooling (0C), the combined acidic aqueous layers were adjusted to pH 7 by addition of solid NaOH, and then extracted with EtOAc (2X50 mL). The combined organic layers were washed with brine (30mL), dried (MgS04), filtered and concentrated in vacuo to give the title compound as a white solid (2.35 g)-LCMS (low pH) RT 0.51 min, m/z (ES) 266 [M+H]+

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CONVERGENCE PHARMACEUTICALS LIMITED; HEER, Jag Paul; CRIDLAND, Andrew Peter; NORTON, David; WO2011/86377; (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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Compound bromo-2-fluoro-3-nitrobenzene 64a (3.1 g, 14.0 mmol), 1-tert-butoxycarbonyl (2S)-2-methylpiperazine(4.2 g, 21.0 mmol) and dioxane (50 mL) were mixed, and tris(bisbenzylideneacetone)palladium (0.6 g,0.7 mmol), 4,5-bisdiphenylphosphino-9,9-dimethyloxaxan (0.8 g, 1.4 mmol) and cesium carbonate (9.1 g, 28 mmol),The reaction was carried out under an argon atmosphere at 110 C for 16 hours. Cool to room temperature, extract with dichloromethane (100 mL¡Á3), and use organic phaseWash with saline solution (100 mL). Dry the organic phase with anhydrous sodium sulfate, remove the desiccant by filtration, and pass the residue through a flash column.Chromatography purification (petroleum ether / ethyl acetate = 5:1) afforded the desired product 1-t-butoxy acyl (2S)-4-(2-fluoro-3-nitrobenzene2-methylpiperazine 64b (2.6 g, 7.7 mmol, red oily liquid), yield: 55%.

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Reference£º
Patent; Nanjing Tianyinjianhua Pharmaceutical Technology Co., Ltd.; Kong Xianglong; Zhou Chao; Zheng Zhixiang; (105 pag.)CN109020957; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics