【药物名称】IDN-1965
化学结构式(Chemical Structure):
参考文献No.38371
标题:C-Terminal modified (N-substd.)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
作者:Bai, X.; Karanewsky, D.S. (Idun Pharmaceuticals, Inc.)
来源:US 5869519; US 5877197; WO 9811129
合成路线图解说明:

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No.46216
标题:Inhibition of apoptosis using interleukin-1beta-converting enzyme (ICE)/CED-3 family inhibitors
作者:Fritz, L.C.; Tomaselli, K.J. (Idun Pharmaceuticals, Inc.)
来源:WO 9810778
合成路线图解说明:

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.

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