【药物名称】UK-1
化学结构式(Chemical Structure):
参考文献No.412306
标题:The novel bis(benzoxazole) cytotoxic natural product UK-1 is a magnesium ion-dependent DNA binding agent and inhibitor of human topoisomerase II
作者:Kerwin, S.M.; et al.
来源:213th ACS Natl Meet (April 13-17, San Francisco) 1997,Abst MEDI 216
合成路线图解说明:

The reaction of 2-amino-3-hydroxy benzoic acid methyl ester (I) with 2-benzyloxybenzoyl chloride (II) by means of pyridine in benzene gives the corresponding amide (III), which is cyclized by heating at 230 C yielding 2-(benzyloxyphenyl)benzoxazole-4-carboxylic acid methyl ester (IV). The hydrolysis of (IV) by means of NaOH in THF/water affords the correponding free acid (V), which is condensed with 2-amino-3-hydroxybenzoic acid methyl ester (I) by means of oxalyl chloride to give the expected amide (VI). Finally, this compound is cyclized by means of p-toluenesulfonic acid in refluxing toluene.

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