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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。

    Preparation of cyclopropanecarboxylic acid esters
    8.
    发明授权
    Preparation of cyclopropanecarboxylic acid esters 失效
    制备环丙烷羧酸酯

    公开(公告)号：US4299972A

    公开(公告)日：1981-11-10

    申请号：US164902

    申请日：1980-07-01

    申请人： Gabor Kovacs ,  Istvan Szekely ,  Marianne Lovasz nee Gaspar ,  Rudolf Soos ,  Joszef Dukai

    发明人： Gabor Kovacs ,  Istvan Szekely ,  Marianne Lovasz nee Gaspar ,  Rudolf Soos ,  Joszef Dukai

    IPC分类号： A01N53/08 ,  A01N53/10 ,  C07B31/00 ,  C07B53/00 ,  C07C67/00 ,  C07C69/743 ,  C07C253/00 ,  C07C255/39 ,  C07D209/49 ,  C07D307/935 ,  C07C67/18

    CPC分类号： C07C69/743

    摘要： A process is disclosed for the preparation of an optically active or racemic cyclopropanecarboxylic acid of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is lower alkyl or halogen;R is a member of a group which contains various cyclic structures as set forth in the specification,the .about. valency bond represents .alpha.- and/or .beta.-configuration;the -- valency bond represents .beta.-configuration,which comprises reacting an optically active or racemic cyclopropanecarboxylic acid of the formula (VII) ##STR2## with a dimethyl-methylidene-ammonium salt of the formula (VIII) ##STR3## wherein X is halogen or lower alkoxy andY.sup.- is a halide or lower alkylsulfate ion in an anhydrous, inert organic solvent, and sebsequently reacting a dimethyl-acloxy-methylidene-ammonium salt thus obtained with an optically active, inactive or racemic alcohol of the formulaR--OHwithout isolation, in the presence of an organic base.

    摘要翻译： 公开了制备式（I）的光学活性或外消旋环丙烷羧酸的方法，其中R 1和R 2相同或不同，各自为低级烷基或卤素; R是包含说明书中所列的各种环状结构的基团的成员，差异化合价键代表α-和/或β-构型; 价键表示β构型，其包括使式（VII）的光学活性或外消旋环丙烷羧酸与式（VIII）的二甲基亚甲基铵盐反应（VIII） ）其中X是卤素或低级烷氧基，Y-是在无水惰性有机溶剂中的卤化物或低级烷基硫酸根离子，然后使由此得到的二甲基 - 酰氧基 - 亚甲基 - 铵盐与光学活性的无活性或外消旋醇反应 式R-OH不分离，在有机碱的存在下。

    Derivatives of bicyclic lactols
    9.
    发明授权
    Derivatives of bicyclic lactols 失效
    双环乳糖的衍生物

    公开(公告)号：US4257962A

    公开(公告)日：1981-03-24

    申请号：US942819

    申请日：1978-09-15

    申请人： Tibor Szabo ,  Laszlo Institoris ,  Gabor Kovacs ,  Gyula Dalmadi ,  Bela Koszegi ,  Istvan Stadler

    发明人： Tibor Szabo ,  Laszlo Institoris ,  Gabor Kovacs ,  Gyula Dalmadi ,  Bela Koszegi ,  Istvan Stadler

    IPC分类号： C07C405/00 ,  A61K31/34 ,  A61K31/343 ,  A61P7/02 ,  A61P25/02 ,  A61P35/00 ,  C07D307/935

    CPC分类号： C07D307/935

    摘要： Racemic or optically active compounds with antitumor activity of the formula: ##STR1## wherein X is oxygen or sulfur;R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkanoyl, benzoyl or phenyl-substituted benzoyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkanoyl;R.sup.3 is C.sub.2 to C.sub.40 straight or branched chain alkyl substituted by hydroxy, epoxy, amino, C.sub.1 to C.sub.6 alkylamino, C.sub.1 to C.sub.6 dialkylamino, C.sub.1 to C.sub.6 alkanoyloxy or, C.sub.1 to C.sub.4 alkoxycarbonyl; cyclohexyl, phenyl unsubstituted or substituted by halogen, amino, C.sub.1 to C.sub.4 alkyl-substituted amino, C.sub.1 to C.sub.4 alkoxy, nitro, or hydroxy; C.sub.1 to C.sub.6 alkanoyl; allyl or phenyl-C.sub.1 to C.sub.4 alkyl unsubstituted or substituted by a C.sub.2 to C.sub.6 alkene group; or where X is sulfur R.sup.3 is as defined above or is C.sub.1 to C.sub.40 straight or branched chain alkyl; and.about. represents the exo- or endo-steric position in the ring and indicates an .alpha.- or .beta.-steric position in the side chain are disclosed.

    摘要翻译： 具有下式的抗肿瘤活性的外消旋或光学活性化合物：其中X是氧或硫; R1是氢，C1至C4烷酰基，苯甲酰基或苯基取代的苯甲酰基; R2是氢或C1-C4烷酰基; R3为C2至C40被羟基，环氧基，氨基，C1至C6烷基氨基，C1至C6二烷基氨基，C1至C6烷酰氧基或C1至C4烷氧基羰基取代的直链或支链烷基; 环己基，未取代或被卤素取代的苯基，氨基，C1至C4烷基取代的氨基，C1至C4烷氧基，硝基或羟基; C1至C6烷酰基; 烯丙基或未被取代或被C2至C6烯基取代的苯基-C1至C4烷基; 或其中X为硫的R 3如上所定义或为C 1至C 40直链或支链烷基; 而DIFFERENCE表示环中的外 - 或内 - 立体位置，并且表示侧链中的α或β-甾族位置。