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天然前列腺素的15-位羟基由于在体内迅速地被前列腺素15-羟基脱氢酶氧化成酮基而失去活性,后来发现若在15位引入甲基则可提高活性,并且作用时间延长. 合成15-甲基前列腺素F_(2a)可用前列腺素F_(2a)为原料经四步反应来完成,也可利用已具有15-酮基的中间体再引入甲基来达到目的.这两种方法均是从已具有前列腺素基本骨架的化合物I或II再引入15-甲基的.我们现在报导一种新的从环戊二烯经十步的合成方法,关键在于将15-位的甲基先引入于接在12位的八碳侧链之中,这样可以省去从前列腺素F_(2a)引进15-甲基的所有反应.
The 15-hydroxyl group of natural prostaglandins, which lost its activity due to its rapid oxidation to keto groups by prostaglandin 15-hydroxydehydrogenase in the body, was subsequently found to increase its activity and prolong the duration of action by introducing methyl groups at position 15. Synthesis 15-methyl prostaglandin F_ (2a) can be used prostaglandin F_ (2a) as the raw material through four steps to complete the reaction can also be used to have a 15-keto-based intermediates to re-introduce the purpose of these two methods All reintroduced 15-methyl from compounds I or II that already had a prostaglandin base skeleton.We now report a novel 10-step synthesis of cyclopentadiene from which the key is to combine the 15-methyl First introduced in the eight carbon chain connected to the 12-bit, thus eliminating the prostaglandin F_ (2a) introduction of 15-methyl all reactions.