3-对甲氧基苯基-1,2,3,4-四氢-1-萘酚的合成

Synthesis of 3-(p-Methoxyphenyl)-1,2,3,4-tetrahydro-1-naphthol

在国内外原有杀它仗合成工艺的基础上,对其起始原料和关键步骤进行了改进,以苯乙酰氯为起始原料,通过酰化反应,成环反应等6步反应,合成了生产第二代香豆素类抗凝血杀鼠剂的重要中间体3 对甲氧基苯基 1,2,3,4 四氢 1 萘酚。总收率(以苯乙酰氯计)达到40%。其中关键的一步成环反应采用多聚磷酸作为环化试剂,避免了使用腐蚀性强酸,从而优化了反应条件,此步反应进行平稳且收率达到82%。

On the basis of earlier synthetic routes of flocoumafen,the starting material was changed and the crucial steps were improved in this route.Using phenylacetyl chloride as starting material,3(pmethoxyphenyl)1,2,3,4tetrahydro1naphthol, which plays an important role in the anticoagulant rodenticides,was synthesized. Including FriedelCrafts acylation and cyclizative condensation,the whole work is made up into 6 steps and the overall yield reached 40%.Instead of using corrosive acids as cyclization reagent,cyclizative condensation was conducted with polyphosphoric acid.The reaction ran smoothly and the yield in this step reached 82%.