Efficient Solid-Phase Synthesis of Diverse 2-Aminoquinazolin-4-ones from Resin-Bound Anilines

摘要

Combinatorial chemistry for the synthesis of non-peptide organic compounds ha emerged as an important tool for drug discovery. Solid-phase synthesis of heterocyclic compounds in particular has been a focus of recent investigations with application toward a variety of drug targets. Among various solid-phase syntheses of heterocycles, we are especially interested in the synthesis of quinazoline-2,4-dione nalogues from resin-bound compounds wit primary amines, incorporating the amines in the rings of the 3N-position of the quinazoline-2,4-dione analogues (Figure 1). In addition to the fact that these solid-phase syntheses can be applicable to a number of resin-bound compounds with primary amines, a compound with a primary amine can be easily derivatized into compounds with various quinazoline-2,4-dione analogues; therefore, the bioactivities of these derivatized compounds can be compared efficiently.