(E)-2-[2-甲氧基-5-(2,4,6-三甲氧基苯乙烯磺酰甲基)]苯胺基乙酸钠的简便合成

Convenient Synthesis of Sodium(E)-2-(5-((2,4,6-trimethoxystyrylsulfonyl)methyl)-2-methoxyphenylamino)-acetate

经6步合成了α,β-不饱和砜类化合物2-[2-甲氧基-5-(2,4,6-三甲氧基苯乙烯磺酰甲基)]苯胺基乙酸,总收率为22%。在关键步骤硫醚氧化步骤中,将反应温度由室温改为75℃,收率由55%提高到85%。缩合脱羧反应中,以醋酸铵为碱,此步收率由30%提高到60%,为该类物质的合成提供了适合较大量合成的方法。

A convenient,reliable and simplified 6-step method for the synthesis of sodium（E）-2-（5-（（2,4,6-trimethoxystyrylsulfonyl）methyl）-2-methoxyphenylamino）-acetate was proposed with the overall yield rate of 22%.In the key step of oxidation,the reaction temperature was changed to 75 ℃ with the increase of yield rate from 55% to 85%.And in condensation,the use of ammonium acetates as the alkali increased the yield rate from 30% to 60%.Such a method could be applied to the mass production of the title product.