Biginelli compounds are one of the most important heterocyclic systems that
play an important role in medicinal chemistry. It has been proved that the biological activities
of these compounds are dependent on the absolute configuration of the C4 atom of
the heterocyclic ring, and thus the oxidative dehydrogenation reaction can affect their biological
and pharmaceutical activities. In this review, the oxidation methods of various
Biginelli compounds have been summarized with a focus on the conditions of the reactions,
the proposed mechanisms, and the effect of the substituents on the reaction.
Keywords: Biginelli reaction, oxidation, dehydrogenation, 2-oxo-1, 2, 3, 4-tetrahydropyrimidine, 2-thioxo-1, 2, 3, 4-tetrahydropyrimidine,
dihydropyrimidinone, pyrimidinone, pyrimidine.
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