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    Process for making bicyclic lactone derivatives for use as intermediates in the synthesis of prostaglandins
    6.
    发明授权
    Process for making bicyclic lactone derivatives for use as intermediates in the synthesis of prostaglandins 失效
    用于制备前列腺素合成中的二环内酯衍生物的方法

    公开(公告)号：US4204999A

    公开(公告)日：1980-05-27

    申请号：US952950

    申请日：1978-10-20

    申请人： Istvan Tomoskozi ,  Gabor Kovacs ,  Istvan Szekely ,  Vilmos Simonidesz ,  Marianna Lovasz nee Gaspar ,  Borbala Keresztesnee Ordog ,  Julia Remport nee Radoczi ,  Istvan Stadler ,  Zsuzsa Visky nee Gombos ,  Csaba Szantay

    发明人： Istvan Tomoskozi ,  Gabor Kovacs ,  Istvan Szekely ,  Vilmos Simonidesz ,  Marianna Lovasz nee Gaspar ,  Borbala Keresztesnee Ordog ,  Julia Remport nee Radoczi ,  Istvan Stadler ,  Zsuzsa Visky nee Gombos ,  Csaba Szantay

    IPC分类号： C07D307/935 ,  C07D493/04 ,  C07D493/02 ,  C07D307/77

    CPC分类号： C07D307/935 ,  C07D493/04

    摘要： A process for the preparation of optically active or racemic lactone diol derivatives of the formula ##STR1## (for use as intermediates in the Corey prostaglandin synthesis). Optically active or racemic lactone diol derivatives are inclosed, in whichR.sup.3 and R.sup.4 are the same or different and stand for a hydrogen, or a lower alkanoyl optionally substituted with one, two or three halogen atoms, or form together a ##STR2## group, in which R.sup.5 and R.sup.6 are the same or different and stand for a hydrogen, alkyl or aryl, with a process for preparing them.According to the invention the above compound are prepared by reacting optically active or racemic lactone of the formula II with formaldehyde or with a formaldehyde polymerisate, in the presence of the mixture of a strong acid and water or of a lower alkane carboxylic acid optionally substituted with one, two or three halogen atoms, and then optionally subjecting the obtained compound of the general formula I, in which R.sup.3 and/or R.sup.4 stand for an alkanoyl optionally substituted with one, two or three halogen atoms to partial or total hydrolysis or alcoholysis in an acid or alkaline medium and/or reacting it with the oxo-compounds of the formula R.sup.5 --CHO or R.sup.6 --CO--R.sup.5 or with the acetals of the above compounds.The compounds according to the invention are useful intermediates in the Corey prostaglandine synthesis.

    摘要翻译： 制备式（IMAGE）的光学活性或外消旋内酯二醇衍生物的方法（用作Corey前列腺素合成中的中间体）。 光学活性或外消旋内酯二醇衍生物被封闭，其中R3和R4相同或不同，代表氢，或任选被一个，两个或三个卤素原子取代的低级烷酰基，或一起形成一个< 其中R5和R6相同或不同，代表氢，烷基或芳基，具有制备它们的方法。 根据本发明，上述化合物通过使式II的光学活性或外消旋内酯与甲醛或甲醛聚合物在强酸和水的混合物或任选被 一个，两个或三个卤素原子，然后任选地使得到的通式I的化合物，其中R 3和/或R 4代表任选被一个，两个或三个卤素原子取代的烷酰基部分或全部水解或醇解 酸或碱性介质和/或使其与式R5-CHO或R6-CO-R5的氧代化合物或与上述化合物的缩醛反应。 根据本发明的化合物在Corey前列腺素合成中是有用的中间体。