Downstream synthetic route of 4629-78-1

4629-78-1, 4629-78-1 3-Methylpiperidin-4-one hydrochloride 22728864, apiperidines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4629-78-1,3-Methylpiperidin-4-one hydrochloride,as a common compound, the synthetic route is as follows.

Preparation of acyl-chloride: A solution of 200 mg (0.571 mmol) of the compound from Example 52A in 4 mL of dichloromethane was initially treated at RT with 249 mu (2.86 mmol) of oxalyl chloride and then with a small drop of DMF.After the reaction mixture had been stirred at RT for 2.5 h, it was concentrated to dryness on a rotary evaporator.The remaining residue was dried under high vacuum and then reacted further in the next substep. Preparation of the amide: The acid chloride obtained above was dissolved in 1 ml of dichloromethane and added to a solution of 171 mg (1.14 mmol) of 3-methylpiperidine-4-one hydrochloride and 398 mu (2.28 mmol) N, N-diisopropylethylamine in 5 ml of dichloromethane dropped.The reaction mixture was stirred at RT for 2 h.After the mixture was concentrated on a rotary evaporator to dryness, the crude product (method 6) was purified by preparative HPLC.After combining the product fractions, evaporation and drying under high vacuum, 236 mg (88% d. Th., 95% purity) of the title compound.

4629-78-1, 4629-78-1 3-Methylpiperidin-4-one hydrochloride 22728864, apiperidines compound, is more and more widely used in various fields.

Reference:
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; HAERTER, MICHAEL; DELBECK, MARTINA; KALTHOF, BERND; LUSTIG, KLEMENS; LINDNER, NIELS; KAST, RAIMUND; WASNAIRE, PIERRE; SUESSMEIER, FRANK; (372 pag.)TW2016/7950; (2016); A;,
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