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本文以取代苯酚为原料,经微波条件下的取代反应和多聚磷酸中进行的环合反应制备了取代色满酮,取代色满酮与甲酸乙酯的缩合产物经氯化反应制备了3-氯代亚甲基色满-4-酮类化合物,共合成了10种未见文献报道的新化合物。化合物结构经质谱和核磁共振氢谱进行了确证,并且采用二倍稀释法对目标化合物的体外抗真菌活性进行了测试,结果表明它们具有很好的体外抗真菌活性,其中化合物4c、4e、4g和4h对石膏样小孢子菌的MIC值为1μg.mL1,高于对照药氟康唑和两性霉素B,具有进一步研究价值。
In this paper, the substituted phenol was used as the raw material, the substituted chromone was prepared by the substitution reaction under microwave irradiation and the cyclization reaction in polyphosphoric acid. The condensation product of chromone and ethyl formate was substituted by chlorination to prepare 3- Chloromethylene chroman-4-one compounds, synthesized a total of 10 kinds of new compounds have not been reported in the literature. The structures of the compounds were confirmed by MS and 1H NMR spectra, and the antifungal activities of the target compounds were tested by double dilution method. The results showed that they have good antifungal activity in vitro. Compounds 4c, 4e, 4g And 4h on the gypsum microsporum MIC value of 1μg.mL1, higher than the control drug fluconazole and amphotericin B, with further research value.