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15-甲基取代的前列腺素(PG)衍生物具有比相应天然PG更强的生理活性和较长的作用时间。其中15-甲基PGP2α甲酯试用于抗早孕和中期引产取得较满意的效果。Yankee曾从光学活性(1B)出发,合成光学活性15-甲基PGP2α甲酯。我们用台成消旋PGF2α的中间体15-酮(1A),参考Yankee的格氏反应条件合成15-甲基醇(2),然后又按PGF2α合成方法,台成15-甲基PGF2α甲酯(5)及其15-差向异构体(6)。
The 15-methyl substituted prostaglandin (PG) derivative has more physiological activity and longer duration of action than the corresponding native PG. 15-methyl PGP2α methyl ester trial of anti-early pregnancy and mid-term induction of labor to obtain more satisfactory results. Yankee has been based on optical activity (1B), the synthesis of optically active 15-methyl PGP2α methyl ester. We synthesized 15-methyl alcohol (2) using the intermediate 15-ketone (1A) of racemic PGF2α with reference to Yankee’s Grignard reaction conditions, and then synthesized 15-methyl PGF2α methyl ester by PGF2α synthesis (5) and its 15-epimer (6).