Ontology highlight
ABSTRACT:
SUBMITTER: Davis TA
PROVIDER: S-EPMC3375951 | biostudies-literature | 2011 Jan
REPOSITORIES: biostudies-literature
Davis Tyler A TA Johnston Jeffrey N JN
Chemical science 20110101 6
The first highly diastereo- and enantioselective additions of aryl nitromethane pronucleophiles to aryl aldimines are described. Identification of an electron rich chiral Bis(Amidine) catalyst for this aza-Henry variant was key to this development, leading ultimately to differentially protected cis-stilbene diamines in two steps. This method then became the lynchpin for an enantioselective synthesis of (-)-Nutlin-3 (Hoffmann-LaRoche), a potent cis-imidazoline small molecule inhibitor of p53-MDM2 ...[more]