3,4,3-LI(1,2-Me-3,2-HOPO)

Chemical Name: N,N'-(1,4-Butylene)bis[N-(1-hydroxy-6-oxo-1,6-dihydropyridin-2-ylcarbonyl)imino]bis(1,3-propylene)bis(3-hydroxy-1-methyl-2-oxo-1,2-dihydropyridine-4-carboxamide)
项目整合开发状态: Preclinical
项目研究机构: University of California, Berkeley (Originator)
合成路线:6-Hydroxypicolinic acid (I) is oxidized to the N-hydroxy pyridinone (II) employing peracetic acid (obtained by mixing Ac2O and H2O2) in the presence of TFA.Protection of the N-hydroxy group of (II) with benzyl chloride affords the N-benzyloxy pyridinone (III).The carboxy group of (III) is then activated as the corresponding acid chloride (IV) by treatment with oxalyl chloride.

合成路线:Acylation of the primary amino groups of spermine (V) by the N acyl thiazolide (VI) furnishes diamide (VII).This is further coupled with acid chloride (IV) producing tetraamide (VIII).Finally,deprotection of the O-benzyl groups under acidic conditions gives rise to the title compound.