EDOXABAN INTERMEDIATE AND PREPARATION METHOD THEREFOR

    公开(公告)号:EP4438592A1

    公开(公告)日:2024-10-02

    申请号:EP22964190.7

    申请日:2022-11-21

    CPC分类号: Y02P20/55

    摘要: The present invention discloses an edoxaban intermediate, and a preparation method therefor. A general structural formula of the edoxaban intermediate is

    or

    wherein R1 is OH, alkoxy or a N,N-dialkyl group, and R2 is hydrogen, alkoxycarbonyl or an amino protecting group. The preparation method includes subj ecting

    and an oxidizing agent to an oxidation reaction to obtain a compound of a formula II; and mixing the compound of the formula II, an aminotransferase, an aminotransferase coenzyme, and a phosphate buffer solution for an enzyme catalyzed reaction or further amine derivatization to obtain a compound of a formula I. Compared with chemical synthesis methods in the prior art, such key edoxaban intermediates and the preparation method therefor provided by the present invention have the advantages of a novel structure, mild reaction conditions, and high yield, having good industrial values.