With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.373604-28-5,tert-Butyl 3-fluoro-4-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.
Sodium bis(trimethylsilyl)amide (0.24 ml_, 1 M in tetrahydrofuran) was added drop-wise to a solution of te/t-butyl 3-fluoro-4-hydroxypiperidine-1-carboxylate (48 mg, 0.22 mmol) in tetrahydrofuran (1 mL) at room temperature. The mixture was stirred for 5 minutes, before it was added drop-wise to a stirred solution of methyl 1-(6-chloro-5- methylpyrimidin-4-yl)indoline-5-carboxylate (60 mg, 0.2 mmol) in tetrahydrofuran (1 mL) at 60 degrees Celsius. The reaction mixture was stirred at 60 degrees Celsius for 2 hours. The reaction mixture was cooled to room temperature and diluted with water and ethyl acetate. The aqueous layer was extracted with ethyl acetate and the combined organic extracts were dried over magnesium sulfate, filtered and the filtrate was concentrated in vacuo. The crude 1-(6-(1-(te/t-butoxycarbonyl)-3-fluoropiperidin-4- yloxy)-5-methylpyrimidin-4-yl)indoline-5-carboxylic acid was used in the next step without purification.
373604-28-5, 373604-28-5 tert-Butyl 3-fluoro-4-hydroxypiperidine-1-carboxylate 42609254, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; PFIZER INC.; DAROUT, Etzer; DENINNO, Michael, Paul; FUTATSUGI, Kentaro; GUIMARAES, Cristiano, Ruch, Werneck; LEFKER, Bruce, Allen; MASCITTI, Vincent; MCCLURE, Kim, Francis; MUNCHHOF, Michael, John; ROBINSON, Ralph, Pelton, Jr.; WO2010/128414; (2010); A1;,
Piperidine – Wikipedia
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