假鹰爪素C衍生物的合成

目的：以活性天然产物假鹰爪素C为先导化合物，合成一系列衍生物，寻找活性优良化合物以及探讨构效关系。方法：以2，4，6-三羟基苯乙酮为起始原料，首先在碱性条件下与碘甲烷反应，而后再与三甲基硅基重氮甲烷反应发生选择性羟基甲醚化，最后一步羟醛缩合反应生成目标产物。结果与结论：合成出6个假鹰爪素C衍生物，尤其是在此类化合物中，既含有互变异构叉还含有F取代得情况下，分别用MS、^1H NMR和^13C NMR鉴定并总结出该类化合物光谱特征。此类含有互变异构化合物的碳谱报道尚属首次。

Synthesis of Analogs of Desmosdumotin C

AIM： To synthesize the analogs of desmosdumotin C with better antitumor activity. MEHTODS： The efficient three-step reaction procedure was employed to prepare analogs of desmosdumotin C. 2, 4, 6-Trihydroxyacetophenone was firstly reacted and then was treated with TMSCHN2 to get the hydroxyl methylation intermediate. Finally, by aldol condensation, the analogs of desmosdumotin C with different substituents on B-ring were prepared by the aldol condensation. RESULTS and CONCLUSION： 6 Analogs of desmosdumotin C were prepared and their structures were identified by MS,^1H NMR and ^13C NMR. The spectral signature of these compounds was summarized, especially for those compounds with tautomers and fluoro suhstitutent. It is the first time to report the ^13C NMR of analogs of desmosdumotin C with their tautomers.