A PROCESS FOR THE PREPARATION OF ISOSERINE DERIVATIVES
    6.
    发明公开
    A PROCESS FOR THE PREPARATION OF ISOSERINE DERIVATIVES 审中-公开
    一种制备异烟碱衍生物的方法

    公开(公告)号:EP2558439A1

    公开(公告)日:2013-02-20

    申请号:EP11718959.7

    申请日:2011-04-13

    申请人: Indena S.p.A.

    IPC分类号: C07C227/32

    摘要: This invention relates to a "one pot" process for the preparation of isoserine derivatives in high diastereoselective way. The process according to the invention includes the steps of reacting a protected glycidic acid with imines to yield isoserines protected both at the -OH and at the -COOH groups, deprotection of the obtained intermediates to isoserines or isoserine 1-4C- alkyl esters. Pure threo derivatives as the main isomer are obtained.

    摘要翻译: 本发明涉及以高选择性方式制备异丝氨酸衍生物的“一锅法”方法。 根据本发明的方法包括使被保护的缩水甘油酸与亚胺反应以产生在-OH和-COOH基团都被保护的异丝氨酸,将所获得的中间体去保护成异丝氨酸或异丝氨酸1-4C-烷基酯的步骤。 获得纯的苏式衍生物作为主要异构体。