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    • 7. 发明授权
    • Preparation of 6-keto-7-oxo-PGF.sub.1.alpha. -derivatives
    • 6-酮-7-氧代-PGF1 + 60 + B衍生物的制备
    • US4429123A
    • 1984-01-31
    • US368016
    • 1982-04-13
    • Istvan TomoskoziIstvan SzekelyKaroly KanaiPeter GyoriGabor Kovacs
    • Istvan TomoskoziIstvan SzekelyKaroly KanaiPeter GyoriGabor Kovacs
    • C07D307/935A61K31/557A61P1/12A61P7/02A61P9/08A61P9/10A61P9/12A61P43/00C07D307/937
    • C07D307/937
    • 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.
    • 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。