纳洛酮为吗啡专一性拮抗剂,临床用为吗啡中毒解救药。本文报道从蒂巴因开始经八步反应合成盐酸纳洛酮的方法。在去氧甲基化反应中采用以三溴化硼为试剂的新工艺;在去氮甲基化反应中,发现了文献上未报道的副产物,通过改变加料方式和试剂配比,避免了副产物的生成。二步改革可使收率显著提高。 Naloxone is morphine-specific antagonist, clinical use of morphine rescue medicine. This article reports the method of synthesizing naloxone hydrochloride from eight steps of reaction of thebaine. In the deoxymethylation reaction using boron tribromide as a reagent of the new process; in the demethylation reaction, the literature has not been reported by-products, by changing the feeding method and reagent ratio, to avoid By-product formation. Two-step reform can yield a significant increase.