Stereospecific sulfoxidation of dibenzo thiepins
    6.
    发明授权
    Stereospecific sulfoxidation of dibenzo thiepins 失效
    二苯并噻吩的立体特异性亚砜化反应

    公开(公告)号:US4334077A

    公开(公告)日:1982-06-08

    申请号:US229223

    申请日:1981-01-28

    IPC分类号: C07D337/14

    CPC分类号: C07D337/14

    摘要: The present invention relates to a process for the preparation of an enantiomer of 7 or 8-fluoro-dibenzo[b,f]thiepin-3-carboxylic acid having a negative rotation and prostaglandin antagonist activity. The process involves preparation and separation of novel diastereoisomeric esters of 10-hydroxy-7 or 8 fluro-dibenzothiepin-3 carboxylic acid ester followed by stereospecific sulfoxidation of the selected diastereoisomer to produce the corresponding novel sulfoxide having a preponderance of the desired configuration of the sulfoxide entity followed by treatment of the product with a strong base to produce directly the desired (-)7 or 8 fluoro-dibenzo[b,f]thiepin-3 carboxylic acid 5-oxide having the structural formula shown below: ##STR1##

    摘要翻译: 本发明涉及制备具有负旋转和前列腺素拮抗剂活性的7或8-氟 - 二苯并[b,f]硫杂-3-羧酸的对映异构体的方法。 该方法包括制备和分离新的非对映异构体的10-羟基-7或8-氟二苯并硫代-3-羧酸酯的酯,然后立即特异性磺化氧化所选的非对映异构体以产生相应的具有优选的亚砜所需构型的亚砜 实体,然后用强碱处理产物,直接生产具有以下结构式的所需的( - )7或8氟二苯并[b,f]硫杂_β-羧酸5-氧化物: