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Condensation between
N-alkyl,
N'-aryl carbo
diimides and malonic acid monoesters leads to a high-yield formation of
N-acyl urea derivativesthat could be cyclized to C-monosubstituted barbiturates by ad
dition of a suita
ble base in a one-pot sequential fashion. In the presence of anelectrophile, the last step gives rise to a one-pot, three-component sequential synthesis of fully substituted barbiturates.