前列腺素类药物关键中间体Corey Lactone的合成工艺研究
The Study on the Synthesis of PGs Ke Intermediate—Corey Lactone

作者: 邓 涛 , 毛 伟 , 陶 春 , 李勤耕 :重庆医科大学,重庆;

关键词: 前列腺素类药物科里内酯手性拆分Prostaglandin Drug Corey Lactone Chiral Separation

摘要:
目前市场上已开发出的前列腺素类似物药物,主要是以Corey lactone关键中间体法进行人工合成。本文以降冰片二烯为原料,经Prins反应,Baeyer-Villiger氧化等一系列反应,成功制成了Corey lactone,并经LC-MS, NMR结构确认;在反应过程中对关键手性中间体进行拆分工艺的研究,最终确认路线中所用到的拆分试剂以及溶剂较其他报道常见且价格低廉,易于工业化生产。

Abstract: Corey lactone is the key intermediate of synthetizing the prostaglandin analogues. In this paper, we use the norbornadiene as the raw material to synthetize the Corey lactone. Through Prins reaction, Baeyer-Villiger oxidation, splitting the chiral intermediate and a series of reaction successfully, the structure has been confirmed by the LC-MS and the NMR. The reagent and the solvent which are used in this method are so common and inexpensive that they can be suitable for industrialized production.

文章引用: 邓 涛 , 毛 伟 , 陶 春 , 李勤耕 (2015) 前列腺素类药物关键中间体Corey Lactone的合成工艺研究。 药物资讯, 4, 15-21. doi: 10.12677/PI.2015.41002

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