GL-406349

Chemical Name: N,N'-Bis[2-[N-[2-(N2,N5-dimethyl-DL-lysylamino)ethyl]carbamoyl]-1H-indol-6-yl]-1H -indole-2,5-dicarboxamide
项目整合开发状态: Preclinical
项目研究机构: Genelabs (Originator)
合成路线:Reaction of methyl 6-nitroindole-2-carboxylate (I) with ethylenediamine (II) in hot DMF gives amino amide (III).After protection of (III) as the N-Boc derivative (IV),catalytic hydrogenation of its nitro group affords amine (V).Indole-2,5-dicarboxylic (VI) is activated as the bis-pentafluorophenyl ester (VII) by treatment with pentafluorophenyl trifluoroacetate.Subsequent coupling between the bis-pentafluorophenyl ester (VII) and amino indole (V) furnishes diamide (VIII).Removal of the N-Boc groups using trifluoroacetic acid in the presence of anisole produces diamine (IX).

合成路线:Coupling of diamine (IX) with the Boc-protected diamino acid (X) by means of DCC and HOBt gives rise to amide (XI).The title compound is finally obtained by acidic cleavage of the N-Boc protecting groups of (XI).