论文部分内容阅读
Corey法合成F型前列腺素是各种合成方法中最受人重视的。此法必经中间体1a,依次转化为2a、2b(或2c)、3b(或3c),然后再引入上侧链而得F型前列腺素(如PGF_(2α))。从1到3须经过三步反应,且1a用Zn(BH_4)_2或硼氢还原得2a时常有副产物生成,有时高达30%,因此,还有不少的还原试剂被利用。Wilson等发现的二异丁基铝氢是一种优良的1,2-加成还原试剂,我们利用这一试剂还原13-烯-15-酮中间体1d,一步就可获得3d,从而简化了合成PGF_(2α)的步骤。
Corey synthesis of prostaglandin F is the most important method in a variety of synthetic methods. This method will be intermediate 1a, 2a, 2b (or 2c), 3b (or 3c), followed by the introduction of the upper side chain F-prostaglandin (such as PGF_ (2α)). From 1 to 3 to go through three steps, and 1a with Zn (BH_4) _2 or borohydride to 2a often produce by-products, and sometimes up to 30%, therefore, there are many reducing agents are used. Diisobutylaluminum hydride, found by Wilson et al., Is an excellent 1,2-addition reducing reagent. By using this reagent to reduce the 13-en-15-one intermediate 1d, 3d can be obtained in a single step, thus simplifying PGF_ (2α) synthesis step.