6,7-亚甲二氧基硫代苯并二氢吡喃-4-酮衍生物的合成及抑菌活性

Synthesis and antifungal activity of 6,7-(methlenedioxy)benzothiopyran-4-one derivatives

以亚甲二氧基苯为起始原料,经过溴化、硫化、环化等反应合成了19个未见文献报道的6,7-亚甲二氧基硫代苯并二氢吡喃-4-酮衍生物,其结构均经核磁共振氢谱和质谱确认。初步抑菌活性测试结果表明,在50 mg/L下,目标化合物对供试7种植物病原菌均有不同程度的抑制作用,其中化合物5b、5i、5k和5l对马铃薯干腐病菌Fusarium solani的抑制率均达75%以上,5h和5i对番茄灰霉病菌Botrytis cinerea的抑制率分别是67.7%和70.4%。

Nineteen 6,7-（methlenedioxy）benzothiopyran-4-one derivatives were synthesized from 1,3-benzodioxole by bromination,sulfuration and cyclization.Their structures were confirmed by 1H NMR and MS.The preliminary bioassay showed that all of the synthesized compounds have different inhibition on seven tested plant pathogenic fungi at the concentration of 50 mg/L.The inhibition rates of compound 5b,5i,5k and 5l against Fusarium solani reached up to 75% and that of compounds 5h and 5i were 67.7% and 70.4% against Botrytis cinerea,respectively.