One-pot synthesis of tri- and di-fluoromethylated bis(indolyl)methanols via Friedel-Crafts-type acylation and alkylation.
Org Biomol Chem
; 20(37): 7491-7498, 2022 09 28.
Article
em En
| MEDLINE
| ID: mdl-36106547
ABSTRACT
A simple and efficient methodology for the first synthesis of tri- and di-fluoromethyl-bis(indolyl)methanols has been demonstrated through a one-pot Friedel-Crafts-type acylation-alkylation of readily available indoles and fluorinated acids. This simple protocol was successfully performed under metal-, additive-, toxic-solvent-, and protective-gas-free conditions, and delivered a wide range of tri- and di-fluoromethyl-bis(indolyl)methanols in moderate to high yields. Notably, this reaction can tolerate diverse vital and reactive functional groups. Furthermore, this one-pot Friedel-Crafts-type acylation-alkylation can be readily expanded to the gram scale with no obvious decrease in the yield, demonstrating its high application potential.
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1
Base de dados:
MEDLINE
Assunto principal:
Metanol
/
Indóis
Idioma:
En
Ano de publicação:
2022
Tipo de documento:
Article