西维来司钠的合成

Synthesis of Sivelestat Sodium

以对羟基苯磺酸钠为原料 ,经 2 ,2 二甲基丙酰氯缩合、与氯化亚砜反应而成 4 ( 2 ,2 二甲基丙酰氧基 )苯磺酰氯 ,再经与 2 氨基苯甲酸缩合、与甘氨酸苄酯成酰胺、加氢脱去保护基团 ,最后与氢氧化钠成盐而合成了西维来司钠。

Sivelestat sodium was synthesized from sodium 4-hydroxy benzosulfonate via condensation with 2,2-dimethyl propionyl chloride, reaction with thionyl chloride to give 4-(2,2-dimethylpropionyloxy)benzenesulfonic chloride which after condensation with 2-aminobenzoic acid, reaction with glycine benzyl ester, hydrogenization, then neutralization with sodium hydroxide.