Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.
ACS Med Chem Lett
; 11(12): 2519-2525, 2020 Dec 10.
Article
en En
| MEDLINE
| ID: mdl-33335676
Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of the clinical candidate AZD9833. The effects of the addition of fluorine on the lipophilicity, permeability, and metabolism are discussed. Many of these changes were tolerated in terms of pharmacology and resulted in high quality molecules which reached advanced stages of profiling in the testing cascade.
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1
Colección:
01-internacional
Banco de datos:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Año:
2020
Tipo del documento:
Article
País de afiliación:
Reino Unido