NEW MATERIAL:A compound of formulaI(R is H, 1-4C alkyl; the wave line shows that hydroxyl bonds to the carbon atoms in the alpha- or beta-configuration; the double bonds between C2 and C3, C13 and C14 are trans) its cyclodextrin clathrate or its salt. EXAMPLE:Methyl 9-oxo-11alpha,15alpha-dihydroxy-16,16-dimethylprosta-trans-2,trans-13- dienoate. USE:It has good uterotonic activity and is used in the feticide of pregnant mammarians, odynopoeia, the synchronization of esterous cycle in female mammarians and in contraseption and menses induction. PREPARATION:The reaction of a cyclopentane derivative of formula II (R4 is 2- tetrahydropyranzyl, 1-ethoxyethyl) with an alkyl phosphonate of formula III (R5 is methyl, ethyl; R6 is alkyl) gives a compound of formula IV, which is hydrolyzed at its ester. Further, the 9alpha-hydroxyl is converted into oxo group, followed by hydrolysis to give the compound of formulaI.
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机译:新材料:式I的化合物(R为H,1-4C烷基;波浪线显示,羟基以α-或β-构型与碳原子相连; C2与C3,C13和C14之间的双键为反式)其环糊精包合物或其盐。实施例:9-氧代-11α,15α-二羟基-16,16-二甲基前体-反式-2,反式-13-二烯酸甲酯。用途:具有良好的子宫收缩作用,可用于孕妇的杀乳剂,痛觉减退,女性哺乳动物的酯化周期同步以及避孕和月经的诱导。制备:式II的环戊烷衍生物(R 4为2-四氢吡喃基,1-乙氧基乙基)与式III的烷基膦酸酯(R 5为甲基,乙基; R 6为烷基)反应得到式Ⅳ化合物,其酯被水解。此外,将9α-羟基转化为氧代基,然后水解以得到式I的化合物。
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