Synthetic studies on an antitumor antibiotic, bleomycin. XIII. Synthesis of 2-formylpyrimidine, a key intermediate for the pyrimidine moiety of bleomycin.

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Abstract
An efficient synthesis of the pyrimidine nucleus of bleomycin was achieved. The reaction of diethoxyacetamidine and ethyl ethoxalylpropionate gave ethyl 2-diethoxymethyl-6-hydroxy-5-methylpyrimidine-4-carboxylate in 76% yield; this product was then converted into ethyl 6-chloro-2-formyl-5-methylpyrimidine-4-carboxylate in 85% yield by treatment with POCl3.