1.
Org Lett
; 18(22): 5780-5783, 2016 11 18.
Artículo
en Inglés
| MEDLINE
| ID: mdl-27934506
RESUMEN
Verubecestat is an inhibitor of ß-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.