3,4,3-LI(1,2-Me-3,2-HOPO)-药物合成数据库

【药物名称】3,4,3-LI(1,2-Me-3,2-HOPO)

化学结构式(Chemical Structure):

参考文献No.	687586
标题:	Synthesis and initial evaluation for in vivo chelation of Pu(IV) of a mixed octadentate spermine-based ligand containing 4-carbamoyl-3-hydroxy-1-methyl-2(1H)-pyridinone and 6-carbamoyl-1-hydroxy-2(1H)-pyridinone
作者:	Xu, J.; Durbin, P.W.; Kullgren, B.; Ebbe, S.N.; Uhlir, L.C.; Raymond, K.N.
来源:	J Med Chem 2002,45(18),3963

合成路线图解说明: 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.

合成路线图解说明: 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.