Angewandte Chemie International Edition · 1998 · 263 citations · 0 references
PharmacyMedicinal ChemistryMicrobiologyDrug DesignDrug DiscoveryStructure-activity RelationshipsMacrocycle SynthesisMacrocyclic Drug DesignChiralityGlycopeptide AntibioticsGlycopeptide SynthesisMethicillin-resistant Staphylococcus Aureus TreatmentThermodynamic Equilibrium ControlThermodynamic Versus Kinetic Control
Controlling the elements of planar and axial chirality are the principal challenges in the synthesis of the aglycon of vancomycin. Vancomycin is the prototypical member of the glycopeptide family of antibiotics which are effective for the treatment of infections by methicillin-resistant Staphylococcus aureus. The first total syntheses of the vancomycin and eremomycin aglycons provide insight into the influence of structure on kinetic and thermodynamic control of atropselective macrocyclizations.