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标题化合物是从Metrodorea stipularis树枝中提取出来的,此化合物具有抗南美洲锥虫病、抗疟疾、抗肿瘤等药理作用。以廉价的2,4,6-三羟基苯乙酮、4-羟基苯甲醛为原料,经吡喃环化、苄基保护酚羟基、羟醛缩合和Pd-C/H2还原不饱和双键及脱保护基,完成天然产物1-(5,7-二羟基-2,2-二甲基苯并吡喃)-3-(2,2-二甲基苯并吡喃)双氢查尔酮的全合成。所有新化合物的结构均经过NMR、IR、HR-MS确认。初步生物活性实验结果表明,1-(5,7-二羟基-2,2-二甲基苯并吡喃)-3-(2,2-二甲基苯并吡喃)双氢查尔酮对大肠杆菌的最小抑菌浓度为32μg/mL。
The title compounds were extracted from the branches of Metrodorea stipularis and have anti-malarial, anti-tumor and other pharmacological effects. With cheap 2,4,6-trihydroxyacetophenone and 4-hydroxybenzaldehyde as raw materials, pyryl cyclization, benzyl protected phenolic hydroxyl, aldol condensation and Pd-C / H2 reduction unsaturated double bond and Deprotection to complete the natural product 1- (5,7-dihydroxy-2,2-dimethylbenzopyran) -3- (2,2-dimethylbenzopyran) dihydrochalcone The total synthesis. The structures of all new compounds were confirmed by NMR, IR and HR-MS. Preliminary bioassay results show that 1- (5,7-dihydroxy-2,2-dimethylbenzopyran) -3- (2,2-dimethylbenzopyran) dihydrochalcone The minimum inhibitory concentration against Escherichia coli is 32 μg / mL.