Microwave‐Assisted Synthesis of Pyrimidine Libraries

Abstract

Abstract Di‐ or trisubstituted pyrimidine libraries are prepared in good yield by the microwave irradiation of an alkynone and either an amidine or guanidine at 120–150 °C in acetonitrile in the presence of sodium carbonate or at 100 °C after treatment with methanolic sodium methoxide in a sealed tube using a monomodal microwave synthesiser. These rapid and efficient methods often require no chromatographic purification and so are appropriate for automated combinatorial methodology and have been applied in the synthesis of a small library of potentially useful novel ligands for the estrogen receptor based on the pyrimidine template.