With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.142374-19-4,tert-Butyl 4-(2-oxoethyl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.
To a solution of methyl 2- (bis (2, 2, 2-trifluoroethoxy) phosphoryl) acetate (1.9 g, 6 mmol) and 18-crown-6 (3.96 g, 15 mmol) in dry THF (70 mL) at -78 was dropwise added KHMDS (15 mL, 7.5 mmol, 0.5 M in toluene) . After stirring at -78 for 0.5h, tert-butyl 4- (2-oxoethyl) piperidine-1-carboxylate (1.14 g, 5 mmol) in dry THF (5 mL) was added to the mixture at -78 and the resulting mixture stirred at rt for 0.5h. The reaction was quenched with saturated aqueous NH4Cl (100 mL) and extracted with DCM (100 mL¡Á3) . The combined organic layers was washed with brine (50 mL) , dried over anhydrous Na2SO4 and concentrated. The residue was purified by chromatography (silica gel: 300-400 mesh, PE/EtOAc 40/1 to 20/1) to afford (Z) -tert-butyl 4- (4-methoxy-4-oxobut-2-enyl) piperidine-1-carboxylate (1.1 g, 78) . LRMS m/z (M-100) 184.1 found, 184.1 required
142374-19-4 tert-Butyl 4-(2-oxoethyl)piperidine-1-carboxylate 10353694, apiperidines compound, is more and more widely used in various.
Reference£º
Patent; MERCK SHARP & DOHME CORP.; RUDD, Michael T.; MENG, Zhaoyang; WAI, Jenny; BENNETT, David Jonathan; BRNARDIC, Edward J.; LIVERTON, Nigel J.; STACHEL, Shawn J.; HAN, Yongxin; TEMPEST, Paul; ZHU, Jiuxiang; XU, Xuewang; (182 pag.)WO2018/68297; (2018); A1;,
Piperidine – Wikipedia
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