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西维来司钠的合成 被引量:7

Synthesis of Sivelestat Sodium
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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%.)
出处 《化学世界》 CAS CSCD 北大核心 2004年第1期29-31,25,共4页 Chemical World
关键词 西维来司钠 合成 弹性蛋白酶抑制剂 急性肺损伤 sivelestat sodium synthesis elastase inhibitor acute lung injury
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  • 2[2]Zeiher B G, Matsuoka S, Kawabata K, et al. Neutrophil elastase and acute lung injury: prospects for sivelestat and other neutrophil elastase inhibitors as therapeutics [J]. Crit Care Med, 2002,30 (5 Suppl ):S281-S287.
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