title: CuAAC macrocyclization: high intramolecular selectivity through the use of copper-tris(triazole) ligand complexes.
abstract: A range of multivalent heteroaryl ligands, copper sources, and solvent systems have been investigated for use in CuAAC-mediated macrocyclization reactions. These studies have revealed the key factors governing selectivity for macrocyclization versus dimerization and identified a simple but specific set of reaction conditions capable of efficiently generating a diverse series of drug-like macrocycles at modest dilution in up to 95% yield.
authors.affiliation: Department of Chemistry, The Scripps Research Institute, La Jolla, California 92014, United States.
authors.forename: Gagan
authors.initials: G
authors.lastname: Chouhan
authors.forename: Keith
authors.initials: K
authors.lastname: James
mesh_terms: D000480:Alkynes / Q000737:chemistry*; D001386:Azides / Q000737:chemistry*; D003300:Copper / Q000737:chemistry*; D003500:Cyclization; D008024:Ligands; D015394:Molecular Structure; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D000480:Alkynes; D001386:Azides; D008024:Ligands; D014230:Triazoles; D003300:Copper