Butadiene derivatives, their preparation and use as an antithrombotic agent
    4.
    发明公开
    Butadiene derivatives, their preparation and use as an antithrombotic agent 失效
    Butadienderivate,ihre Herstellung und Verwendung als antithrombotisches Mittel。

    公开(公告)号:EP0563798A1

    公开(公告)日:1993-10-06

    申请号:EP93104977.9

    申请日:1993-03-25

    摘要: Novel butadiene derivatives of the formula [I]:

    wherein Ring A is tri-lower alkoxyphenyl, R¹ and R² combine each other to form a group of the formula:



            〉N-R³



    or one of R¹ and R² is lower alkoxy, and the other is group of the formula: -NHR³, in which R³ is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted amino, hydroxy or pyridylcarbonyl, or salts thereof.
    Among the desired butadiene derivatives [I] of the present invention, the 3-butenoic acid-type compounds per se have antithrombotic activity, but they can also be used as an intermediate for preparing the 2,5-pyrrolidinedione-type compounds having excellent antithrombotic activity. And additionally a butenoic acid ester of the formula [II]:

    wherein Ring A is a tri-lower alkoxyphenyl group, and one of R¹² and R²² is a lower alkoxy group, and the other is hydroxy group, or a salt thereof, as synthetic intermediate.

    摘要翻译: 式[I]的新型丁二烯衍生物:其中环A是三低级烷氧基苯基,R 1和R 2彼此结合形成下式的基团:其中R 1和R 3之一或 R 1和R 2是低级烷氧基,另一个是式-NHR 3的基团,其中R 3是氢,取代或未取代的低级烷基,取代或未取代的低级烷氧基,取代的 或未取代的氨基,羟基或吡啶基羰基,或其盐。 在本发明的所需丁二烯衍生物[I]中,3-丁烯酸类化合物本身具有抗血栓形成活性,但也可以用作制备具有优异抗血栓形成的2,5-吡咯烷二酮型化合物的中间体 活动。 另外,式[II]的丁烯酸酯:其中环A是三低级烷氧基苯基,R 1和R 2之一是低级烷氧基 ,另一种是羟基,或其盐作为合成中间体。

    Method for removing the protecting group for hydroxy group
    8.
    发明公开
    Method for removing the protecting group for hydroxy group 失效
    维尔法伦,嗯,伊朗geschützteHO-Gruppe freizumachen。

    公开(公告)号:EP0567949A1

    公开(公告)日:1993-11-03

    申请号:EP93106643.5

    申请日:1993-04-23

    摘要: A method for removing tri-substituted silyl group from β-lactam compound having a tri-substituted silyl group-protecting hydroxy group, which comprises treating with an acid and a fluoride selected from alkali metal fluoride, alkaline earth metal fluoride and hydrogenfluoride of organic or inorganic amine, by which the tri-substituted silyl group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.

    摘要翻译: 一种从具有三取代甲硅烷基保护羟基的β-内酰胺化合物中除去三取代甲硅烷基的方法,该方法包括用酸和选自碱金属氟化物,碱土金属氟化物和氟化氢的有机或 无机胺,通过其可以在中等条件下容易且有效地除去三取代甲硅烷基,从而可以低成本高收率地获得所需化合物。

    Dicarboxylic acid derivatives and process for preparation thereof
    9.
    发明公开
    Dicarboxylic acid derivatives and process for preparation thereof 失效
    Dicarbonsäurederivateund Verfahren zu deren Herstellung。

    公开(公告)号:EP0519738A1

    公开(公告)日:1992-12-23

    申请号:EP92305647.7

    申请日:1992-06-19

    摘要: Disclosed are a dicarboxylic acid compound represented by the formula (I):

       wherein R represents hydrogen atom, a lower alkyl group, phenyl group or hydroxyl group; R¹ represents a straight or branched alkyl group having 1 to 10 carbon atoms or a lower alkyl group substituted by a group selected from aryl group, a sulfur- or nitrogen-containing heterocyclic monocyclic group and a cycloalkyl group having 4 to 8 carbon atoms; R² represents a substituted or unsubstituted aryl group, a cycloalkyl group having 4 to 8 carbon atoms or a sulfur-containing or nitrogen-containing heterocylcic group; X represents sulfur atom, oxygen atom or a substituted or unsubstituted imino group; Y¹ represents imino group, oxygen atom or sulfur atom and Y² represents nitrogen atom, or Y¹ represents a vinylene group and Y² represents a group: -CH=; m represents 0 to 3; and n represents 0 or 1,
    an ester thereof or pharmaceutically acceptable salts thereof, and a process for preparing the same.

    摘要翻译: 公开了由式(I)表示的二羧酸化合物:其中R表示氢原子,低级烷基,苯基或羟基; R 1表示具有1〜10个碳原子的直链或支链烷基或被选自芳基,含硫或含氮杂环单环基团和具有4-8个碳原子的环烷基取代的低级烷基 原子; R 2表示取代或未取代的芳基,具有4-8个碳原子的环烷基或含硫或含氮杂环基; X表示硫原子,氧原子或取代或未取代的亚氨基; Y 1表示亚氨基,氧原子或硫原子,Y 2表示氮原子,或Y 1表示亚乙烯基,Y 2表示-CH =; m表示0〜3; 和n表示0或1,其酯或其药学上可接受的盐及其制备方法。