新型镇痛药AF-353的合成

Synthesis of New Analgesic Drug AF-353

以1-(2-羟基-5-甲氧基)乙-1-酮为反应原料,经6步反应制得关键中间体2-(5-碘-2-异丙基-4-甲氧基苯氧)乙腈(8),再与Bredereck试剂、盐酸苯胺和碳酸胍经"一锅法"合成新型镇痛药AF-353,总收率55%,其结构经~1H NMR和MS确证。

The key intermediate,2-（5-iodo-2-isopropyl-4-methoxyphenoxy） acetonitrile（8）,was prepared by six-step reaction using 1-（2-hydroxy-5-methoxyphenyl） ethan-1-one as the starting material.The antagonist AF-353 with total yield of 55% was synthesized by one-pot multi component reaction with Bredereck＇s reagent,aniline hydrochloride and guanidine carbonate. The structure was confirmed by-1H NMR and MS.