Deloxolone sodium, ISF-2715
地洛索龙 Chemical Name: 3beta-Hydroxyolean-9(11)-en-30-oic acid hydrogen succinate disodium salt; 3beta-(3-Carboxypropionyloxy)olean-9(11)-en-30-oic acid disodium salt; (3beta,20beta)-3-(3-Carboxy-1-oxoporpoxy)olean-9(11)-en-29-oic acid disodium salt
CAS No. 68635-51-8, 68635-50-7 (free acid)
项目整合开发状态: Biological Testing
项目研究机构: ISF (Originator)
合成路线:The oxidation of 3-beta-acetoxyolean-12-en-30-oic acid methyl ester (I) with H2O2 in hot acetic acid gives 3beta-acetoxy-12-oxoolean-30-oic acid methyl ester (II),which is treated with Br2 in 40% HBr acetic acid yielding 3beta-acetoxy-12-oxoolean 9-en-30-oic acid methyl ester (III).The reduction of (III) with hydrazine and sodium ethoxide in ethanol affords 3beta-hydroxyolean-9(11)-en-30-oic acid (IV),which is finally esterified with succinic anhydride (V) in hot pyridine.
📌 参考资料/链接：
参考文献标题:3beta-Hydroxy-18beta-olean-9-en-30-oic acids
文献作者:Pifferi,G.; Umani Ronchi,A.; Farina,C.; Gamba,A.(ISF SpA)
参考来源:DE 2811253; FR 2383909; GB 1575494; JP 78116363; US 4173648
📄 详细内容
合成路线:The oxidation of 3-beta-acetoxyolean-12-en-30-oic acid methyl ester (I) with H2O2 in hot acetic acid gives 3beta-acetoxy-12-oxoolean-30-oic acid methyl ester (II),which is treated with Br2 in 40% HBr acetic acid yielding 3beta-acetoxy-12-oxoolean 9-en-30-oic acid methyl ester (III).The reduction of (III) with hydrazine and sodium ethoxide in ethanol affords 3beta-hydroxyolean-9(11)-en-30-oic acid (IV),which is finally esterified with succinic anhydride (V) in hot pyridine.
参考文献标题:Deloxolone sodium
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1986,11(8),643
产品链接: CAS No.68635-50-7››