HYBUTIMIBE INTERMEDIATE AND PREPARATION METHOD THEREFOR

The present invention provides a hybutimibe intermediate and a preparation method therefor. The method comprises the steps of: reacting an easily available raw material of p-fluorobenzoyl butyrate with cheap sulfonylhydrazine to obtain sulfonylhydrazone valerate, then reacting sulfonylhydrazone vale...

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Hauptverfasser: CHEN, Yanan, CHEN, Lei, WANG, Xiaoming, ZHANG, Yuncai, LI, Xufei, ZHOU, Yaqian, WU, Jinlong, ZHANG, Yong, JIN, Meichun, XU, Xiaojie, ZHAN, Dongkai
Format: Patent
Sprache:chi ; eng ; fre
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Zusammenfassung:The present invention provides a hybutimibe intermediate and a preparation method therefor. The method comprises the steps of: reacting an easily available raw material of p-fluorobenzoyl butyrate with cheap sulfonylhydrazine to obtain sulfonylhydrazone valerate, then reacting sulfonylhydrazone valerate with carbon dioxide under an alkaline condition to obtain a compound of formula VI with a Z configuration, followed by subjecting the compound of formula VI to acylation, reduction and hydrolysis to obtain the hybutimibe intermediate of (Z)-5-(4-fluorophenyl)-6-hydroxy-hex-4-enoic acid. The preparation method involves readily available and cheap raw materials, has mild reaction conditions, simple and safe operation, a good stereoselectivity, a high yield and low costs, and is suitable for industrial mass production. La présente invention concerne un intermédiaire d'hystéétimibe et son procédé de préparation. Le procédé comprend les étapes consistant : à faire réagir une matière première facilement disponible d