Preparation method of cis-chiral 3-fluoro-4-hydroxypiperidine and derivative of cis-chiral 3-fluoro-4-hydroxypiperidine

The invention discloses a preparation method of a cis-chiral 3-fluoro-4-hydroxypiperidine derivative as shown in a formula (I), which comprises the following steps: starting from trans-chiral 3-fluoro-4-hydroxypiperidine and a derivative thereof, oxidizing into carbonyl or dihydroxyl, and further re...

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Hauptverfasser: SU XING, YU FENG, FENG HONGWEI, LU SHOUFU, YAN FEIJUN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a preparation method of a cis-chiral 3-fluoro-4-hydroxypiperidine derivative as shown in a formula (I), which comprises the following steps: starting from trans-chiral 3-fluoro-4-hydroxypiperidine and a derivative thereof, oxidizing into carbonyl or dihydroxyl, and further reducing to generate the cis-chiral 3-fluoro-4-hydroxypiperidine derivative. The method disclosed by the invention is good in yield, few in treated and purified impurities, controllable and capable of being directly used for next-step reaction, the operation is simplified, meanwhile, the preparation process can be ensured to be more environment-friendly, and mass production can be realized to meet the production of medicinal raw materials. 本发明公开了一种如式(I)所示的顺式手性3-氟-4-羟基哌啶衍生物的制备方法,通过从反式手性3-氟-4-羟基哌啶及其衍生物出发,经过氧化成羰基或双羟基,进一步还原生成顺式手性3-氟-4-羟基哌啶衍生物。本发明的方法收率好,处理及纯化杂质少、可控、可直接用于下一步反应,简化的操作同时可以保证制备过程中更具绿色环保,可以大量生产来满足医药原料药的生产。