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    Preparation of N-6 demethylated, 9,10-dihydrolysergic acid alkyl esters
    1.
    发明公开
    Preparation of N-6 demethylated, 9,10-dihydrolysergic acid alkyl esters 审中-公开
    Zubereitung von N-6-demethylierten 9,10-DihydrolysergsäureAlkylestern

    公开(公告)号：EP2113504A1

    公开(公告)日：2009-11-04

    申请号：EP08155371.1

    申请日：2008-04-29

    申请人： LEK Pharmaceuticals d.d.

    发明人： The designation of the inventor has not yet been filed

    IPC分类号： C07D457/02 ,  C07D457/04 ,  C07D457/06 ,  A61K31/48 ,  A61P25/00

    CPC分类号： C07D457/04 ,  C07D457/02 ,  C07D457/06

    摘要： A process for producing N -6 demethylated 9,10-dihydrolysergic acid alkyl ester is described, which comprises a step of N -6 demethylation of 9,10-dihydrolysergic acid alkyl esters with chloroformate and wherein the N -6 demethylation step is performed in the presence of an organic catalyst. Further, a process for converting a compound of formula I (DHLSAIkyI) into a compound of formula II (DHLSAIkyI-F) comprises the steps of: providing (and maintaining) a reaction medium free of water and/or HCI, and reacting DHLSAIkyI with chloroformate in said reaction medium free of water and/or HCI, to obtain the compound of formula II (DHLSAIkyI-F).

    摘要翻译： 描述了一种制备N-6脱甲基化9,10-二氢赖氨酸烷基酯的方法，其包括用氯甲酸酯将9,10-二氢赖氨酸烷基酯N -6脱甲基化的步骤，其中N -6去甲基化步骤在 存在有机催化剂。 此外，将式I化合物（DHLSAIkyI）转化为式II化合物（DHLSAI1I-F）的方法包括以下步骤：提供（和维持）不含水和/或HCl的反应介质，并使DHLSAIkyI与 所述反应介质中不含水和/或HCl，得到式II化合物（DHLSAIky-F）。