Intermediates and methods of preparation of intermediates in the enantiomeric synthesis of (20R)homocamptothecins and the enantiomeric synthesis of (20R)homocamptothecins
    8.
    发明授权
    Intermediates and methods of preparation of intermediates in the enantiomeric synthesis of (20R)homocamptothecins and the enantiomeric synthesis of (20R)homocamptothecins 失效
    (20R)同型喜树碱的对映体合成中的中间体和(20R)高卡波品的对映体合成中间体的制备方法

    公开(公告)号:US06723853B2

    公开(公告)日:2004-04-20

    申请号:US09940059

    申请日:2001-08-27

    IPC分类号: C07D49114

    摘要: A method of synthesizing a compound having the formula: from a compound having the formula: wherein R1 is hydrogen, fluorine, chlorine or SiR5R6R7, wherein R5, R6, and R7 are independently the same or different an alkyl group or an aryl group, R2 is an alkyl group, R3 is a protecting group, R4 is an alkyl group, an allyl group, a propargyl group —CO2H, or a benzyl group, R8 is —CO2R10, wherein R10 is an alkyl group or an aryl group, X1 is OH and X2 is H, includes the step of exposing compound (III) to at least one of an organic acid or an inorganic acid. A compound has the general formula (III).

    摘要翻译: 合成具有下式的化合物的方法:具有下式的化合物:其中R 1是氢,氟,氯或SiR 5 R 6 R 7,其中R 5, 6>,R 7独立地相同或不同,是烷基或芳基,R 2是烷基,R 3是保护基,R 4是烷基, 烯丙基,炔丙基-CO 2 H或苄基,R 8为-CO 2 R 10,其中R 10为烷基或芳基,X 1为OH且X 2为 是H,包括将化合物(III)暴露于有机酸或无机酸中的至少一种的步骤。 化合物具有通式(III)。