The novel solution-phase synthesis of an array of biologically relevant benzimidazoles in a
simple two-step procedure is revealed. Transformations are carried out in excellent yield by
condensation of mono-Boc protected ortho-phenylene diamine and supporting Ugi
reagents. Subsequent acid treatment and evaporation affords benzimidazoles in good to
excellent yield. The described protocol represents a highly attractive solution-phase
procedure for the rapid generation of benzimidazole libraries.

The novel solution-phase synthesis of an array of biologically relevant quinoxalinones in a
simple two-step procedure is revealed. Transformations are carried out in excellent yield by
condensation of mono-Boc protected ortho-phenylene di-amine, glyoxylic acids and
supporting Ugi reagents. Subsequent acid treatment and evaporation affords
quinoxalinones in good to excellent yields.