Abstract

Treatment of [1,3,5]triazine-2,4,6-tricarboxylic acid triethyl ester ( 4 ) with arylhydrazines provided 5-amino-6-oxo-1,6-dihydro[1,2,4]triazine-3-carboxylic acid ethyl esters 5a– g in moderate to good yields. Hydrolysis under basic conditions gave the corresponding free carboxylic acids 6a– d . Despite the relatively high number of heteroatoms present the amido as-triazine compounds 6a– d showed good solubility in phosphate buffer as determined by a lyophilization solubility assay. Building block 5a served as starting point for the syntheses of two discrete exocyclic 5-amido and 3-amido compound libraries 7 and 8 , respectively.

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