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    Preparation of 6-keto-7-oxo-PGF.sub.1.alpha. -derivatives
    1.
    发明授权
    Preparation of 6-keto-7-oxo-PGF.sub.1.alpha. -derivatives 失效
    6-酮-7-氧代-PGF1 + 60 + B衍生物的制备

    公开(公告)号：US4429123A

    公开(公告)日：1984-01-31

    申请号：US368016

    申请日：1982-04-13

    申请人： Istvan Tomoskozi ,  Istvan Szekely ,  Karoly Kanai ,  Peter Gyori ,  Gabor Kovacs

    发明人： Istvan Tomoskozi ,  Istvan Szekely ,  Karoly Kanai ,  Peter Gyori ,  Gabor Kovacs

    IPC分类号： C07D307/935 ,  A61K31/557 ,  A61P1/12 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D307/937

    CPC分类号： C07D307/937

    摘要： The present invention relates to a process for the preparation of compounds of the general Formula I ##STR1## (wherein A is a straight or branched chain alkylene group having 1-5 carbon atoms;B is ethylene, Z or E vinylene, or ethynylene;R.sup.1 stands for hydrogen, an alkyl group having 1-5 carbon atoms or a pharmaceutically acceptable cation;R.sup.2 is hydrogen, an alkanoyl group having 1-5 carbon atoms or aroyl;R.sup.3 is hydrogen or methyl;R.sup.4 is a straight or branched chain alkyl group having 1-8 carbon atoms or an optionally monosubstituted aryloxymethyl group;R.sup.5 stands for hydrogen or an alkyl group having 1-5 carbon atoms)which comprises oxidizing a compound of the Formula III, IV or V ##STR2## or a mixture thereof R.sup.6 is hydrogen or an alkyl or alkanoyl group having 1-5 carbon atoms with a mild electrophilic oxidizing agent and if desired reacting the compound of the Formula I thus obtained wherein R.sup.5 is hydrogen with an alkanol containing 1-5 carbon atoms in the presence of boron trifluoride etherate in a manner known per se to yield the corresponding compound of the Formula I in which R.sup.5 is an alkyl group having 1-5 carbon atoms.

    摘要翻译： 本发明涉及制备通式Ⅰ（I）化合物的方法（其中A是具有1-5个碳原子的直链或支链亚烷基; B是乙烯，Z或E亚乙烯基， 或亚乙炔基; R 1表示氢，具有1-5个碳原子的烷基或药学上可接受的阳离子; R 2是氢，具有1-5个碳原子的烷酰基或芳酰基; R 3是氢或甲基; R 4是直链或 具有1-8个碳原子的支链烷基或任选的单取代的芳氧基甲基; R 5代表氢或具有1-5个碳原子的烷基），其包括将式III，IV或V的化合物（III （V）或其混合物R6是氢或具有1-5个碳原子的烷基或烷酰基，具有温和的亲电氧化剂，如果需要，则使式I的化合物反应 其中R5是含有1-5个碳原子的链烷醇 原子在三氟化硼乙醚合物存在下，以本身已知的方式得到相应的式I化合物，其中R 5为具有1-5个碳原子的烷基。

    Process for making bicyclic lactone derivatives for use as intermediates in the synthesis of prostaglandins
    3.
    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。

    2,3,4-Trinor-m-inter-phenylene-prostaglandin derivatives and compositions and method for inhibiting blood platelet aggregation
    6.
    发明授权
    2,3,4-Trinor-m-inter-phenylene-prostaglandin derivatives and compositions and method for inhibiting blood platelet aggregation 失效
    2,3,4-三硝基间亚苯基前列腺素衍生物及其抑制血小板聚集的组合物和方法

    公开(公告)号：US4451483A

    公开(公告)日：1984-05-29

    申请号：US367068

    申请日：1982-04-09

    申请人： Istvan Szekely ,  Krisztina Kekesi ,  Mariann Lovasz nee Gaspar ,  Sandor Botar ,  Pal Hadhazy ,  Istvan Rakoczi ,  Laszlo Muszbek ,  Judit Skopal ,  Istvan Stadler ,  Karoly Horvath ,  Gabor Kovacs ,  Peter Kormoczy

    发明人： Istvan Szekely ,  Krisztina Kekesi ,  Mariann Lovasz nee Gaspar ,  Sandor Botar ,  Pal Hadhazy ,  Istvan Rakoczi ,  Laszlo Muszbek ,  Judit Skopal ,  Istvan Stadler ,  Karoly Horvath ,  Gabor Kovacs ,  Peter Kormoczy

    IPC分类号： A61K31/5575 ,  C07C405/00 ,  C07D307/937 ,  A61K31/34 ,  C07D307/935

    CPC分类号： C07D307/937 ,  C07C405/00 ,  C07C405/0041 ,  Y10S514/822

    摘要： 2,3,4-trinor-1,5-inter-m-phenylene-prostacycline derivatives of the formula (I), ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1-4 alkyl group, an alkali metal cation or a primary, secondary, tertiary or quaternary ammonium cation,R.sup.2 and R.sup.3 each represent hydrogen or a C.sub.1-4 alkanoyl, benzoyl, substituted benzoyl, tetrahydropyranyl, ethoxyethyl or tri-(C.sub.1-4 alkyl)-silyl group,R.sup.4 is hydrogen or a C.sub.1-4 alkyl group, andR.sup.5 is a hexyl, heptyl, phenoxymethyl or m-trifluoromethylphenoxymethyl group, orR.sup.5 represents a group of the general formula ##STR2## and in this latter formula Z is an amino group or an optionally halo-substituted C.sub.1-4 alkanoylamino, benzoylamino or tosylamino group, andR.sup.6 is a C.sub.4-6 alkyl, phenyl or benzyl group,are prepared by reacting a bicyclic lactol of the formula (II), ##STR3## with a reactive phosphorane prepared from a triphenyl-m-carbobenzylphosphonium halide and a strong base, optionally esterifying the resulting prostaglandin derivative and, whenever it contains a free amino group, protecting this amino group by acylation, reacting then the prostaglandin derivative with an electrophilic reagent of the formula E-X, wherein X is halogen atom and E is halogen atom or an acetyl, trifluoroacetyl or N-succinimido group, and subjecting the resulting halogenated PGI.sub.1 derivative to hydrogen halide elimination. The compounds of the formula (I) possess valuable biological effects and can be applied in therapy primarily as blood platelet aggregation inhibiting agents.

    摘要翻译： 式（I）的2,3,4-三硝基-1,5-间 - 间 - 亚苯基 - 前列环素衍生物，其中R 1是氢，C 1-4烷基，碱金属阳离子或 伯，仲，叔或季铵阳离子，R2和R3各自表示氢或C1-4烷酰基，苯甲酰基，取代的苯甲酰基，四氢吡喃基，乙氧基乙基或三（C1-4烷基） - 甲硅烷基，R4是氢或 C 1-4烷基，R 5为己基，庚基，苯氧基甲基或间三氟甲基苯氧基甲基，或R 5表示通式“IMAGE”的基团，在后一式中Z为氨基或任意卤素取代的C1 -4烷酰基氨基，苯甲酰氨基或甲苯磺酰氨基，R6是C4-6烷基，苯基或苄基，是通过使式（II）的双环内酰醇与式（II）的双环内酰醇与由 三苯基-m-苄基苄基卤化鏻和强碱，任选地酯化所得的前列腺素衍生物，并且每当其含有时 游离氨基，通过酰化保护该氨基，然后将前列腺素衍生物与式EX的亲电试剂反应，其中X是卤素原子，E是卤素原子或乙酰基，三氟乙酰基或N-琥珀酰亚胺基，并使 得到的卤化PGI1衍生物消除卤化氢。 式（I）化合物具有有价值的生物学效应，可用作主要作为血小板聚集抑制剂的治疗。

    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。