西维来司钠的合成  

Synthesis of Sivelestat Sodium

作　　者：李伟[1] 卞红平[1] 宁奇[1] 

机构地区：[1]上海医药工业研究院,上海200040

出　　处：《化学世界》2004年第1期29-31,25,共4页Chemical World

摘　　要：以新戊酰氯为原料,经酯化、酰氯化、酰胺化、脱苄基,与氢氧化钠成盐制成西维来司钠,1,经工艺改进,多步收率有较大提高,总收率47.9%。N-(2-氨基苯甲酰基)甘氨酸苄酯(4),4是以对甲苯磺酸、甘氨酸、苯甲醇为原料,经酯化、酰胺化、还原制得,总收率91.7%。Sivelestat sodium was synthesized from pivaloyl chloride via esterification, acyl chloridization amidation, debenzylation, and then salt formation. The reaction conditions were improved and the total yield was 47.9%. _N_-(2-aminobenzoyl) glycine benzyl ester(4), 4 was synthesized from _p_-toluenesulfonic acid, glycine and benzyl alcohol via esterification, amidations and reduction with an overall yield of (91.7%.)

关 键 词：西维来司钠 合成 弹性蛋白酶抑制剂 急性肺损伤 

分 类 号：TQ226.36[化学工程—有机化工]