• Chemistry, Medicine
  • Published in
    Journal of combinatorial…
    2009
  • DOI:10.1021/cc800106h

Parallel synthesis of 2-aryl-4-aminobenzimidazoles and their evaluation as gonadotropin releasing hormone antagonists.

@article{Green2009ParallelSO,
  title={Parallel synthesis of 2-aryl-4-aminobenzimidazoles and their evaluation as gonadotropin releasing hormone antagonists.},
  author={Daniel Michael Green and Igor Goljer and Diane S Andraka and Murty V. Chengalvala and Linda K Shanno and Warren Hurlburt and Jeffrey C. Pelletier},
  journal={Journal of combinatorial chemistry},
  year={2009},
  volume={11 1},
  pages={
          117-25
        }
}
2-Trifluoromethyl-4-aminobenzimidazoles were previously identified by screening to be active antagonists of the gonadotropin releasing hormone receptor (GnRH-R). Structure activity relationships and diversity oriented synthesis are shown here in greater detail. 2-Substituted benzimidazoles were synthesized in parallel by the coupling of carboxylic acids with a latent intermediate diamine monomer to yield the desired benzimidazoles in fair yields. A catch and release strategy was employed as a… CONTINUE READING