A chemo- and regioselective C6-functionalization of 2,3-disubstituted indoles: highly efficient synthesis of diarylindol-6-ylmethanes.
Org Biomol Chem
; 17(13): 3462-3470, 2019 03 27.
Article
em En
| MEDLINE
| ID: mdl-30888364
ABSTRACT
An organocatalytic chemo- and regioselective C6-functionalization of 2,3-disubstituted indoles has been established via a reaction with ortho-hydroxybenzyl alcohols, which afforded biologically important diarylindol-6-ylmethanes in overall high yields (up to 99% yield). This protocol not only provides an efficient method for constructing biologically important diarylindol-6-ylmethane frameworks in an atom economical fashion, but also serves as a good example for the direct catalytic C6-functionalization of indoles, which have been rarely investigated. More importantly, the preliminary biological evaluation revealed that this new class of diarylindol-6-ylmethanes exhibited strong cytotoxicity to HeLa cell lines.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
Org Biomol Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
China