Final Activity Report Summary - GMNL2003LACTAM (Atropenantioselective lactamisations using an intramolecular Staudinger ligation strategy)
An intramolecular Staudinger ligation strategy has been disclosed to ring-closed biaryl-type macrolactams. Various ring size of biaryl-macrolactames have been efficiently prepared. In particulary, a 16-membered o,o-dimethyl substituted biaryl containing a medium-sized lactam has been prepared featuring axial chirality as the only asymmetric element. The same product was also prepared using an enantiomerically enriched P-chiral auxiliary but without any detectable asymmetric induction. This researcher has allowed the development of a powerful intramolecular Staudinger ligation strategy to ring-close biaryl-type macrolactams.