METAL-CATALYZED ASYMMETRIC 1,4-CONJUGATE ADDITION OF VINYLBORON COMPOUNDS TO 2-SUBSTITUTED-4-OXY- CYCLOPENT-2-EN-1-ONES YIELDING PROSTAGLANDINS AND PROSTAGLANDIN ANALOGS
    4.
    发明公开
    METAL-CATALYZED ASYMMETRIC 1,4-CONJUGATE ADDITION OF VINYLBORON COMPOUNDS TO 2-SUBSTITUTED-4-OXY- CYCLOPENT-2-EN-1-ONES YIELDING PROSTAGLANDINS AND PROSTAGLANDIN ANALOGS 审中-公开
    金属催化的不对称乙烯基有机硼化合物的1,4-共轭加成2-取代的4-氧基 - 环戊-2-烯-1-酮与前列腺素和前列腺素类似物的高产

    公开(公告)号:EP3166918A1

    公开(公告)日:2017-05-17

    申请号:EP15819728.5

    申请日:2015-07-09

    CPC classification number: C07F7/1892 C07F5/025 C07F7/1804

    Abstract: This invention provides a novel method for the preparation of 2,3-disubstituted -4-oxy-cyclopentan1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted -4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

    Abstract translation: 本发明提供了一种新颖的方法,用于制备2,3-二取代的-4-氧基 - 环戊烷-1-酮的化合物是没有为前列腺素的合成和前列腺素产业关联的类似物是有用的。 该方法包括金属催化的不对称1,4-共轭加成乙烯基硼酸化合物的2- substituiertem -4-氧环戊-2-烯-1-酮。 此方法依赖于使用毒性较低,容易处理的试剂,并可以比一些常规方法提供的更温和的条件下进行,得到2,3-二取代的-4-氧基 - 环戊烷-1-酮的化合物和对映体非对映选择性 ,这是前体以高收率的所述前列腺素和前列腺素类似物。

    A PROCESS FOR THE PREPARATION OF REGADENOSON
    6.
    发明公开
    A PROCESS FOR THE PREPARATION OF REGADENOSON 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON REGADENOSON

    公开(公告)号:EP3080139A1

    公开(公告)日:2016-10-19

    申请号:EP13899097.3

    申请日:2013-12-10

    CPC classification number: C07H19/16 C07H19/167

    Abstract: The present invention provides novel processes for the preparation of regadenoson having the formula (I). In some embodiments, the intermediates for the synthesis of regadenoson are also provided.

    Abstract translation: 本发明提供了制备具有式(I)的regadenoson的新方法。 在一些实施方案中,还提供了用于合成regadenoson的中间体。

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