Solid-Phase Convergent Synthesis of a Benzimidazolone Library via the Combination of Two Smaller Arrays of Carboxylic Acids and Secondary Amines

The concept of convergent synthesis can be extended to combinatorial chemistry in order to obtain collections of products characterized by considerable chemical diversity and a certain molecular complexity. In this work, a library consisting of three carboxylic acids containing a benzimidazolonic functionality with variations at two positions was synthesized on solid phase. After cleavage, this library was combined with a second library consisting of 16 solid-supported amines containing two points of variation. IRORI technology was used for the split-and-mix synthesis of the final 48 members library.