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    PROCESS FOR PREPARATION OF 7-OXABICYCLO 2.2.1]HEPT-5-ENE-2-CARBOXYLIC ACID DERIVATIVES
    1.
    发明公开
    PROCESS FOR PREPARATION OF 7-OXABICYCLO 2.2.1]HEPT-5-ENE-2-CARBOXYLIC ACID DERIVATIVES 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON 7-OXABICYCLO¬2.2.1HEPT-5-EN-2-CARBONSÄURE-DERIVATEN

    公开(公告)号：EP1319662A1

    公开(公告)日：2003-06-18

    申请号：EP01965636.2

    申请日：2001-09-14

    申请人： Kuraray Co., Ltd. ,  SAGAMI CHEMICAL RESEARCH CENTER

    发明人： KUWAYAMA, Tomoya, c/o KURARAY CO., LTD ,  UJITA, Katsuji, c/o KURARAY CO., LTD ,  SHIMIZU, Kazuya, c/o KURARAY CO., LTD ,  TERASHIMA, Shiro

    IPC分类号： C07D493/08

    CPC分类号： C07D493/08

    摘要： The present invention provides a method of industrially advantageously producing 7-oxabicyclo[2.2.1]hept-5-ene-2-carboxylic acid derivatives under mild conditions in a high yield. The present invention relates to a production method of a 7-oxabicyclo[2.2.1]hept-5-ene-2-carboxylic acid derivative of the formula (III) or the formula (IV), which comprises reacting an α,β-unsaturated carboxylic acid of the formula (I) with a furan derivative of the formula (II) in the presence of a Lewis acid:
    wherein each symbol is as defined in the specification.

    摘要翻译： 本发明提供了一种工业上有利地以高产率在温和条件下生产7-氧杂双环-2,2-庚-5-烯-2-羧酸衍生物的方法。 本发明涉及式（III）或式（IV）的7-氧杂双环-2,2-庚-5-烯-2-羧酸衍生物的制备方法，其包括使α，β-不饱和羧酸 式（I）与式（II）的呋喃衍生物在路易斯酸：CHEM的存在下反应，其中每个符号如说明书中所定义.a

    PROCESS FOR PRODUCING (5 ALPHA, 7 ALPHA)-3-SPIRO-2'-(1',3'-DIOXOLAN)-24-OXOCHOLEST-22-EN-7-YL BENZOATE
    2.
    发明公开
    PROCESS FOR PRODUCING (5 ALPHA, 7 ALPHA)-3-SPIRO-2'-(1',3'-DIOXOLAN)-24-OXOCHOLEST-22-EN-7-YL BENZOATE 审中-公开
    生产（5α，7α）-3-螺-2' - （1'，3'-二氧杂环己烷）-24-氧代青霉烷-22-烯-7-基苯甲酸酯的方法

    公开(公告)号：EP1837343A1

    公开(公告)日：2007-09-26

    申请号：EP05814172.2

    申请日：2005-12-07

    申请人： KURARAY CO., LTD.

    发明人： KOYAKUMARU, Kenichi, c/o KURARAY CHEMICAL CO., LTD ,  UJITA, Katsuji, c/o KURARAY CO., LTD

    IPC分类号： C07J21/00

    CPC分类号： C07J21/00

    摘要： The present invention provides a method of producing (5α,7α)-3-spiro-2'-(1',3'-dioxolan)-24-oxocholest-22-en-7-yl benzoate represented by the formula (I)

    including dissolving a crude product containing (5α,7α)-3-spiro-2'-(1',3'-dioxolan)-24-oxocholest-22-en-7-yl benzoate, which is obtained by a reaction step, in methanol within the range of 1.5 - 3 in a mass ratio relative to the contained (5α,7α)-3-spiro-2'-(1',3'-dioxolan)-24-oxocholest-22-en-7-yl benzoate to give a solution, adding the solution to water within the range of 5 - 30 in a mass ratio relative to the contained (5α,7α)-3-spiro-2'-(1',3'-dioxolan)-24-oxocholest-22-en-7-yl benzoate to solidify (5α,7α)-3-spiro-2'-(1',3'-dioxolan)-24-oxocholest-22-en-7-yl benzoate to give a suspension, separating the solid from the suspension, and drying the obtained solid.
    The compound obtained by the present invention is useful as a production intermediate for squalamine having potent antibacterial activity and antitumor activity.

    摘要翻译： 本发明提供了由式（I）表示的（5α，7α）-3-螺-2' - （1'，3'-二氧戊环）-24-氧代胆甾-22-烯-7-基苯甲酸酯的制备方法， 包括溶解通过反应步骤获得的含有（5α，7α）-3-螺-2' - （1'，3'-二氧戊环）-24-氧代胆甾-22-烯-7-基苯甲酸酯的粗产物， 在相对于所含（5α，7α）-3-螺-2' - （1'，3'-二氧戊环）-24-氧代胆甾-22-烯-7-醇的质量比为1.5-3的范围内的甲醇中， （5α，7α）-3-螺-2' - （1'，3'-二氧戊环） - 甲醇的质量比为5〜30的范围内的水， （5α，7α）-3-螺-2' - （1'，3'-二氧戊环）-24-氧代胆甾-22-烯-7-基苯甲酸酯向 给出悬浮液，从悬浮液中分离固体，并干燥所得固体。 本发明获得的化合物可用作具有有效抗菌活性和抗肿瘤活性的角鲨胺的制备中间体。