1 research outputs found
Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer’s Disease
Verubecestat is an inhibitor of β-secretase
being evaluated
for the treatment of Alzheimer’s disease. The first-generation
route relies on an amide coupling with a functionalized aniline, the
preparation of which introduces synthetic inefficiencies. The second-generation
route replaces this with a copper-catalyzed C–N coupling, allowing
for more direct access to the target. Other features of the new route
include a diastereoselective Mannich-type addition into an Ellman
sulfinyl ketimine and a late-stage guanidinylation