Cyanoacetic acid → n-(6-Amino-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-2-cyanoacetamide

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Reaction Steps

5,6-Diamino-1,3-dimethyluracil hydrate is reacted with cyanoacetic acid to yield 5-cyanoacetamido-6-amino-1,3-dimethyluracil of the formula: ##STR4## The 5-cyanoacetamido-6-amino-1,3-dimethyluracil is treated with sodium hydroxide within a temperature range of 145°-155° C. to yield 8-carboxymethyltheophylline of the formula: ##STR5## The 8-carboxymethyltheophylline is treated with an alkylated inhibitor of the formula: ##STR6## to yield the compounds of formula (II).

Provenance & Evidence