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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,既含有互变异构又还含有F取代得情况下,分别用MS、1HNMR和13CNMR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。
OBJECTIVE: To synthesize a series of derivatives with the active natural product, false hawking paw C, as the lead compound, to search for excellent active compounds and to explore the structure-activity relationship. METHODS: 2,4,6-trihydroxyacetophenone was used as the starting material, firstly reacted with methyl iodide under alkaline conditions, and then reacted with trimethylsilyl diazomethane to produce selective hydroxymethyl etherification. The final aldol condensation produces the desired product. RESULTS AND CONCLUSION: Six compounds of Fake Tomato C were synthesized, especially in these compounds, which contain both tautomerism and F substitutions. They were identified by MS, 1HNMR and 13CNMR, respectively. Spectral characteristics of these compounds. It is the first time that such carbon spectra containing tautomeric compounds have been reported.