Downstream synthetic route of 1215071-17-2

1215071-17-2 tert-Butyl 3,3-difluoro-4-oxopiperidine-1-carboxylate 56776981, apiperidines compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1215071-17-2,tert-Butyl 3,3-difluoro-4-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

tert-butyl 4-(2-ethoxy-2-oxoethylidene)-3,3-dimethylpiperidine-1-carboxylate At 0 C., to a solution of ethyl (diethoxyphosphoryl)formate (950 mg, 4.52 mmol) in THF (50 mL) was added sodium hydride (102 mg, 4.25 mmol) at 0 C. The resulting mixture was stirred for 15 min and then was added by tert-butyl 3,3-difluoro-4-oxopiperidine-1-carboxylate (798 mg, 3.39 mmol) at 0 C. The reaction mixture was stirred for 0.5 h at 0 C., warmed up to room temperature and stirred for 3 h at room temperature. When the reaction was done, it was quenched by the addition of water (20 mL). The resulting mixture was extracted with ethyl acetate (40 mL*3). The organic phases were combined, washed with brine and dried over Na2SO4. The solvent was removed under reduced pressure and the residue was purified by flash chromatography eluting with EtOAc in petroleum ether (0% to 50% gradient) to yield tert-butyl 4-(2-ethoxy-2-oxoethylidene)-3,3-dimethylpiperidine-1-carboxylate as colorless oil (560 mg, 35%). MS: m/z=205.9 [M-100+1]+., 1215071-17-2

1215071-17-2 tert-Butyl 3,3-difluoro-4-oxopiperidine-1-carboxylate 56776981, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Merck Patent GmbH; SHERER, Brian A.; BRUGGER, Nadia; LAN, Ruoxi; CHEN, Xiaoling; (60 pag.)US2019/23687; (2019); A1;,
Piperidine – Wikipedia
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