西维来司钠的合成

Synthesis of Sivelestat Sodium

以甘氨酸苄酯对甲苯磺酸盐为起始原料 ,经与 2 -硝基苯甲酰氯缩合、还原 ,得 N- (2 -氨基苯甲酰基 )甘氨酸苄酯 ,继而与 4 - (2 ,2 -二甲基丙酰氧基 )苯磺酰氯缩合 ,再经脱苄基、成盐制得西维来司钠 ,总收率 5 6 .9%。

Sivelestat sodium was synthesized from glycine benzyl ester p -toluenesulfonate by condensation with 2-nitrobenzoyl chloride, and reduction to afford N -(2-aminobenzoyl)glycine benzyl ester, followed by condensation with p -pivaloyloxybenzenesulfonyl chloride, debenzylation and salt formation. The overall yield was 56.9%.