Synthesis method of chiral piperidinol derivative

The invention relates to a synthesis method of a chiral nitrogen-substituted piperidinol derivative, which comprises the following steps of: carrying out condensation reaction on N-protected 3-oxopiperidine serving as an initial raw material and fatty aldehyde with hydroxyl and amino active groups t...

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Hauptverfasser: HE YAWEN, CHEN BIN, CHEN DEXIANG, MA LIANGXIU, CHENG JIANFENG, XIA JIANSHENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to a synthesis method of a chiral nitrogen-substituted piperidinol derivative, which comprises the following steps of: carrying out condensation reaction on N-protected 3-oxopiperidine serving as an initial raw material and fatty aldehyde with hydroxyl and amino active groups to obtain a compound II, carrying out asymmetric reduction on the compound II to obtain a compound III, and carrying out asymmetric reduction on the compound III to obtain a compound I, the synthesis route of the chiral piperidine derivative is # imgabs0. According to the invention, N-substituted piperidine-3-ketone is used as an initial raw material, carbonyl reacts with aliphatic aldehyde under protection or unprotection to generate an olefin product, and the olefin product is subjected to asymmetric hydrogenation reduction to obtain the chiral piperidine derivative. The method is simple in process, mild in reaction condition and high in chiral catalyst selectivity, and a qualified high-purity target product can b