纳屈酮系纳洛酮类似物,为吗啡受体拮抗剂,它比纳洛酮有更强的生物活性和更长的作用时间,因此我们合成了纳屈酮。以14-羟基二氢降吗啡酮为中间体与溴代环丙甲烷在DMF中直接反应制得纳屈酮,收率59％。反应时间从1周缩短为1d。重要中间体14-羟基二氢降吗啡酮是以蒂巴因为原料,通过六步反应而制得。其中还原一步收率提高6％。 The naltrexone-based naloxone analog, a morphine receptor antagonist, has more biological activity and longer duration of action than naloxone, so we synthesized naltrexone. Nalidronone was synthesized by direct reaction of 14-hydroxy dihydromorphorone with bromocyclopropane in DMF. The yield was 59%. The reaction time shortened from 1 week to 1d. Important intermediates 14-hydroxy-2-dihydro-2-nororphistone is based on the raw material of Tiba, obtained through a six-step reaction. One step reduction in yield by 6%.