Novel 2-aryl indole hNK1 receptor ligands were prepared utilising palladium cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK1 receptor binding affinity and good brain penetration (e.g., 9d) were synthesised.
Department of Medicinal Chemistry, Merck, Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Harlow, Essex, UK. kevin_dinnell@merck.com
