A PRACTICAL SYNTHESIS OF 1-ALKYL-3-AMINO-4-ARYL-1,8-NAPHTHYRIDIN-2-(1H)-ONE,A PARTIAL STRUCTURE OF ACAT INHIBITOR SMP-797

摘要

3-Amino-4-[3-(3-benzyloxypropoxy)phenyl]-1-butyl-1,8-naphthyridin-2(1H)-one,which is a naphthyridine part of a potent ACAT (acyl-CoA: cholesterol acyltransferase) inhibitor SMP-797,was effectively synthesized from m-bromophenol in 5 steps without isolating intermediates.The synthesis involved the intramolecular aldol reaction as a key step.