Practical Gram Scale Asymmetric Catalysis with Boroxinate Brempty setnsted Acids Derived from the VAPOL and VANOL Ligands

Our laboratories have been engaged in utilizing catalysts derived from the VAPOL and VANOL ligands towards the development of efficient asymmetric processes over the last several years. Subsequent to their development, practical scale-up of these methodologies to gram scale has always been deemed necessary to demonstrate. This article will report on such successful grain scale asymmetric catalysis that has been realized in our laboratories using the boroxinate Brempty setnsted acid catalysts derived from the VAPOL and VANOL ligands. The processes reviewed will be the catalytic asymmetric aziridination of imines and the direct catalytic asymmetric aminoallylation of aldehydes.