Polymer Supported Synthesis of Multi-substituted Pyrimidine-4-one Derivatives via Pbf-activated Thio

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Efficient polymer supported synthesis of multi-substituted pyrimidine-4-one derivatives was described.Target products were produced from fluorenylmethoxycarbonyl(Fmoc) protected β-amino acid loaded on hydroxymethyl resin through deprotection, N-alkylation, guanidine formation, and cleavage of 2,2,4,6,7-pentamethyl dihydrobenzofuran-sulfonyl(Pbf) by trifluoracetic acid(TFA) followed with cyclization. The procedure has the advantages of easy operation, mild reaction conditions, and forming multiple substituents.
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