Aqueous Benzylic C-H Trifluoromethylation for Late-Stage Functionalization.
J Am Chem Soc
; 140(39): 12378-12382, 2018 10 03.
Article
em En
| MEDLINE
| ID: mdl-30247886
ABSTRACT
The installation of trifluoromethyl groups has become an essential step across a number of industries such as agrochemicals, drug discovery, and materials. Consequently, the rapid introduction of this critical functional group in a predictable fashion would benefit current practitioners in those fields. This communication describes a mild trifluoromethylation of benzylic C-H bonds with high selectivity for the least hindered hydrogen atom. The reaction provides monotrifluoromethylation and proceeds in an environmentally friendly acetone/water solvent system. The method can be used to install benzylic trifluoromethyl groups on highly functionalized drug molecules.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tolueno
/
Derivados de Benzeno
/
Hidrocarbonetos Fluorados
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article