Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer's Disease.
Org Lett
; 18(22): 5780-5783, 2016 11 18.
Article
en En
| MEDLINE
| ID: mdl-27934506
ABSTRACT
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.
Buscar en Google
Banco de datos:
MEDLINE
Asunto principal:
Tiadiazinas
/
Ácido Aspártico Endopeptidasas
/
Óxidos S-Cíclicos
/
Secretasas de la Proteína Precursora del Amiloide
/
Enfermedad de Alzheimer
Límite:
Humans
Idioma:
En
Revista:
Org Lett
Asunto de la revista:
BIOQUIMICA
Año:
2016
Tipo del documento:
Article