化学学报 ›› 1980, Vol. 38 ›› Issue (5): 451-458. 上一篇    下一篇

论文

抗昆虫保幼激素类似物的合成

甘立宪, 郭广忠, 徐锦文   

  1. 中国科学院上海有机化学研究所
  • 投稿日期:1978-10-18 发布日期:2013-06-03

THE SYNTHESIS OF THE INSECT ANTIJUVENILE HORMONE ANALOGS

GAN LI-XIAN, GUO GUANG-ZHONG, XU JIN-WEN   

  1. Shanghai Insti tute of Organic Chemistry, Academia Sinica
  • Received:1978-10-18 Published:2013-06-03

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 the search of potent precocene analogs possessing antijuvenile hormone activity,some new chromeno derivatives were synthesized.In the presence of polyphosphorio acid,the pyrogallol monomethyl ether 4 reaoted with β,β-dimethylacrylio acid(5) to afford the ohromanone(6),whioh was reduced with lithium aluminum hydride in ether,followed by the acid-catalysed dehydration to give the desired product 8.'hreatment 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.