INTERMEDIATE OF EDOXABAN TOSYLATE AND PREPARATION METHOD THEREFOR

Disclosed are an intermediate of edoxaban tosylate and a preparation method therefor, having the advantages that the preparation process is simple, reaction conditions are mild, the cost is low, and raw materials are easy to obtain. The method comprises the synthesis steps of: subjecting a compound...

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Bibliographic Details
Main Authors LIU, Shengmin, HU, Kai, LI, Yonggang, FAN, Jinmin, GAO, Shizhao, MEI, Yijiang
Format Patent
LanguageChinese
English
French
Published 22.06.2023
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:Disclosed are an intermediate of edoxaban tosylate and a preparation method therefor, having the advantages that the preparation process is simple, reaction conditions are mild, the cost is low, and raw materials are easy to obtain. The method comprises the synthesis steps of: subjecting a compound N-methyl-4-piperidone, as a raw material, to a substitution reaction with bromine to generate a compound represented by formula (II); subjecting the compound represented by formula (II) to a thiolation reaction with sodium sulfide to obtain a compound represented by formula (III); subjecting the compound represented by formula (III) to a cyclization reaction with glyoxylic acid to obtain a compound represented by formula (IV); subjecting the compound represented by formula (IV) to an esterification reaction with alcohol to obtain a compound represented by formula (V), and then reacting to obtain a compound represented by formula (VI), or directly reacting the compound represented by formula (IV) under the effect of
Bibliography:Application Number: WO2021CN139089