Reviw of synthetic methods of imiquimod was made.From 4-hydroxy-2-(1H)-quinolinone,imiquimod(Ⅵ) was obtained in good yield through 6 steps procedure.In the substituting reaction of Ⅴ and benzylamine,Ⅷ was formed instead of Ⅶ if DMF is employed as a solvent.Also,Ⅷ was the only product when Ⅴ,ammonia and DMF were mixed and heated.The debenzylation of Ⅶ was not successful at the condition used.%在对咪喹莫特的合成方法综述的基础上,以4-羟基-2-(1H)-喹啉酮为原料经硝化、氯代、胺取代、还原、环合、胺取代共六步反应合成了咪喹莫特。该过程适合于大规模操作。在以苄胺取代化合物Ⅴ的4-位氯原子时,如以DMF为溶剂,则所得化合物不是Ⅶ而是Ⅷ。同样,以氨的DMF溶液与Ⅴ反应时也得到Ⅷ。Ⅶ的脱苄反应在所用的试验条件下未能发生。
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