| 摘要 |
<p><P>PROBLEM TO BE SOLVED: To provide a method for conveniently synthesizing Sivelestat, a human neutrophil elastase inhibitor to be applied to treating acute pneumonia accompanying a systemic inflammatory response syndrome. <P>SOLUTION: The method of preparing Sivelestat (1), 2-(2-(4-(pivaloyloxy)phenylsulfonamido)benzamido)acetic acid, includes starting from sodium 4-hydroxybenzenesulfonate and isatoic anhydride. The method is conducted without isolating most intermediates and is particularly advantageous in terms of yields and productivity. Furthermore, the resulting Sivelestat is highly pure and can be conveniently transformed into Sivelestat sodium tetrahydrate. <P>COPYRIGHT: (C)2011,JPO&INPIT</p> |
