论文部分内容阅读
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。
In order to find a precocious analogue with anti-juvenile hormone activity, we synthesized several new oxa-naphthalene derivatives with similar structure and precocious hormone for biological testing. Pyrogallol-1-methyl ether (4) is condensed with an excess of β, β-dimethylacrylic acid (5) to form the corresponding chromone (6) in the presence of polyphosphoric acid followed by reduction with lithium aluminum hydride And hydrochloric acid for catalytic dehydration, to obtain the desired products 8.8, respectively, with dimethyl sulfate, propyne bromine and methyl isocyanate to give the analogues 10,11 and 12. Biological activity tests for compounds 8, 10, 11, 12 are underway.