【摘要】 为寻找有抗保幼激素活性的早熟素类似物,我们合成了几个新的、结构与早熟素相似的氧杂萘衍生物供生物试验筛选。在多聚磷酸存在下,使焦棓酚-1-甲醚(4)与过量的β,β-二甲基丙烯酸(5)缩合生成相应的色满酮(6),然后经锂铝氢还原及盐酸催化脱水,即得所需产物8.8分别再与硫酸二甲酯,丙炔溴及异氰酸甲酯反应便可得类似物10、11和12。化合物8、10、11、12的生物活性试验正在进行中。更多还原

【Abstract】 In the search of potent precocene analogs possessing antijuvenile hormone activity, some new chromene derivatives were synthesized. In the presence of polyphosphoric acid, the pyrogallol monomethyl ether 4 reacted with β, β-dimethylacrylic acid (5) to afford the chromanone (6), which was reduced with lithium aluminum hydride in ether, followed by the acid-catalysed dehydration to give the desired product 8. Treatment of 8 with dimethyl sulfate, propargyl bromide and methyl isocyanate gave the compounds 10, 11 and 12 respectively. The biological tests of these four compounds (8, 10, 11 and 12) will be reported elsewhere.更多还原