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青蒿素为我国首先发现的新型抗疟药。合成定位标记的青蒿素对药物在体内分布、代谢以及抗疟作用原理的研究将起很大作用。我们选择C_(15)-甲基~(14)C标记的青蒿素作为合成目的物以合成[~(14)C]-青蒿素。青蒿降解成一双酮化合物,再经三步反应可得一中间体酮酯化合物,后者与~(14)CH_3I反应可得标记原子引入化合物中,然后再经八步反应即可得[~(14)C]-青蒿素。目
Artemisinin is the first antimalarial drug discovered in our country. Synthetic localization markers of artemisinin in the distribution of drugs in the body, the role of anti-malarial metabolism and research will play a significant role. We chose C_ (15) - methyl ~ (14) C - labeled artemisinin as a synthetic target to synthesize [~ (14) C] - artemisinin. Artemisia annua decomposed into a ketone compound, and then through a three-step reaction to obtain an intermediate ketone ester compound, the latter with ~ (14) CH_3I reaction can be labeled atoms introduced into the compound, and then after eight steps to get [~ (14) C] - Artemisinin. Head