IDN-1965
3-[2(S)-(1,3-二甲基-1H-吲哚-2-酰羧酰胺)-3-甲基丁胺]-5-氟-4-氧戊二醇酸Chemical Name: 3-[N-(1,3-dimethyl-1H-indol-2-ylcarbonyl)-L-valylamino]-5-fluoro-4-oxopentanoic acid; 3-[2(S)-(1,3-Dimethyl-1H-indol-2-ylcarboxamido)-3-methylbutanamido]-5-fluoro-4-oxopentanoic acid
CAS No. 204919-14-2
项目整合开发状态: Preclinical
项目研究机构: Idun (Originator)
合成路线:Coupling of 1,3-dimethylindole-2-carboxylic acid (II) with 5-fluoro-4-hydroxy-3-(valinylamino)pentanoic acid tert-butyl ester (I) using EDC in the presence of DMAP furnished amide (III).Subsequent Swern oxidation of the hydroxyl group of (III) gave ketone (IV).The tert-butyl ester of (IV) was finally cleaved by treatment with trifluoroacetic acid.
📌 参考资料/链接：
参考文献标题:C-Terminal modified (N-substd.)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
文献作者:Bai,X.; Karanewsky,D.S.(Idun Pharmaceuticals,Inc.)
参考来源:US 5869519; US 5877197; WO 9811129
📄 详细内容
合成路线:Coupling of 1,3-dimethylindole-2-carboxylic acid (II) with 5-fluoro-4-hydroxy-3-(valinylamino)pentanoic acid tert-butyl ester (I) using EDC in the presence of DMAP furnished amide (III).Subsequent Swern oxidation of the hydroxyl group of (III) gave ketone (IV).The tert-butyl ester of (IV) was finally cleaved by treatment with trifluoroacetic acid.
参考文献标题:Inhibition of apoptosis using interleukin-1beta-converting enzyme (ICE)/CED-3 family inhibitors
文献作者:Fritz,L.C.; Tomaselli,K.J.(Idun Pharmaceuticals,Inc.)
参考来源:WO 9810778
产品链接: CAS No. 204919-14-2››