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 hydro- xymet...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 hydro- xymethyl resin through deprotection, N-alkylation, guanidine formation, and cleavage of 2,2,4,6,7-pentamethyl dihy-drobenzofuran-sulfonyl(Pbf) by trifluoracetic acid(TFA) followed with cyclization. The procedure has the advantages of easy operation, mild reaction conditions, and forming multiple substituents.展开更多
基金Supported by the Scientific Forefront and Interdisciplinary Innovation Project of Jilin UniversityChina(No.421031531412)+1 种基金the Jilin Provincial Research Foundation for Basic Research China(No.3D109K856604)
文摘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 hydro- xymethyl resin through deprotection, N-alkylation, guanidine formation, and cleavage of 2,2,4,6,7-pentamethyl dihy-drobenzofuran-sulfonyl(Pbf) by trifluoracetic acid(TFA) followed with cyclization. The procedure has the advantages of easy operation, mild reaction conditions, and forming multiple substituents.