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青蒿素(1)是从青蒿中分离到的一个具有独特结构的抗疟新药.它的结构包含一个C—O—O—C基团并连接着C—O—C—O—C的交替排列,这种特殊的结构可能与其抗疟活性有关.我们曾用青蒿酸(2)进行光敏氧化,经由⊿~5-烯-4-氢过氧化物3合成了天然青蒿素B(4).因而若从5得3的双氢化合物6,再经臭氧化和内分子缩酮反应,似可在C_4和C_6位之间架一个过氧桥,从而得到一个类似青蒿素结构的化合物.根据这一设想,我们已成功地合成了这个化合物.具有这种独特结构的过氧化物还是首次被合成.
Artemisinin (1) is a unique antimalarial drug isolated from Artemisia annua L. Its structure consists of a C-O-O-C group linked to C-O-C-O-C Alternate arrangement, this particular structure may be related to its anti-malarial activity.We have used the artemisinic acid (2) for photosensitive oxidation via ⊿ ~ 5-ene-4-hydroperoxide 3 Synthesis of natural artemisinin B 4) Thus, if 5 from 5 to 6 of the hydrogen compound 6, and then by ozonation and internal molecular ketal reaction, it seems possible to frame an overhead bridge between C_4 and C_6, resulting in an artemisinin-like structure of the compound Based on this idea, we have successfully synthesized this compound, and the peroxide with this unique structure is the first to be synthesized.