HS-1141

Chemical Name: 4-[4-(3-Aminobenzoisoxazol-6-yloxy)butoxy]-N,N-diisopropyl-3-methoxybenzamide
项目整合开发状态: Biological Testing
项目研究机构: Dong-Wha (Originator), Pusan National University (Originator)
合成路线:Treatment of 4-hydroxy-3-methoxybenzoic acid (I) with thionyl chloride and then with diisopropyl amine provided amide (II).Alkylation of (II) with 1,4-dibromobutane and potassium carbonate in acetonitrile,followed by treatment with sodium iodide afforded iodobutylether (III).Then,alkylation of 2-fluoro-4-hydroxybenzonitrile (IV) with iodide (III) in the presence of sodium hydride in DMF gave (V),which was condensed with acetone oxime (VI) and potassium tert-butoxide to provide (VII).Finally,cyclization of (VII) in a refluxing hydroalcoholic solution of HCl generated the target benzisoxazole.
📌 参考资料/链接:
参考文献标题:3-Amino-1,2-benzisoxazoles: A new family of potent inhibitors of LTB4 binding to the human neutrophils
文献作者:Suh,H.; et al.
参考来源:Bioorg Med Chem Lett 1997,7(4),389