Parallel synthesis is a powerful tool for hit and lead optimization in medicinal chemistry; however, it has traditionally been utilized for a limited set of synthetic transformations (amide coupling, S<sub>N</sub>Ar, reductive amination, etc.) that have resulted in narrowly populated chemical space.  The development of new reactions and sequences compatible with library synthesis can dramatically enhance our ability to efficiently access molecular space that was previously prohibitively complex.  Here we describe an amidine formation / oxidative cyclization sequence for the parallel synthesis of benzimidazoles from widely available aniline building blocks.  This method allows rapid variation of the benzimidazole C4-C7 vectors and tolerates a broad range of pharmaceutically-relevant functional groups.  The expansion of scope to include the synthesis of aza-benzimidazoles from aminopyridines will also be presented.

Parallel synthesis of benzimidazoles via oxidative cyclization

2019 Fall National Meeting

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