title: Expedient Synthesis of N1-Substituted Triazole Peptidomimetics.
abstract: A general procedure for the rapid diversification of peptide scaffolds is described. A one-pot click reaction between a peptide-alkyne and a series of in situ generated aryl/alkyl azides affords novel N1-substituted triazole peptidomimetics. This transformation is of broad scope, operates under mild conditions, and is parallel chemical synthesis compatible.
authors.affiliation: Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Steven B
authors.initials: SB
authors.lastname: Coffey
authors.affiliation: Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.|Pfizer Worldwide Medicinal Chemistry , 610 Main Street , Cambridge, Massachusetts 02139, United States.
authors.forename: Gary
authors.initials: G
authors.lastname: Aspnes
authors.affiliation: Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Allyn T
authors.initials: AT
authors.lastname: Londregan
mesh_terms: D000480:Alkynes / Q000737:chemistry; D001386:Azides / Q000737:chemistry; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry; D057786:Peptidomimetics / Q000138:chemical synthesis* / Q000737:chemistry; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D000480:Alkynes; D001386:Azides; D010455:Peptides; D057786:Peptidomimetics; D014230:Triazoles
keywords: mild conditions; one-pot click reaction; parallel synthesis; rapid diversification; triazole peptidomimetics