Synthesis and pharmacological screening of some N-carboxymethylbarbituric acid derivatives. I.

Reaction of haloacetate with barbital and methylphenobarbital in polar aprotic solvents in the presence of anhydrous K2CO3 gave N-carboalkoxymethyl derivatives in good yields. Acidic hydrolysis of the latter compounds affords N-carboxymethyl derivatives of barbital 8 or methylphenobarbital 7. From acid 7 and 8 via acid chlorides, amides 11--20 were prepared. These amides lack anticonvulsant activity and show only slight sedative and analgesic action.