One-Pot Synthesis of Trifluoromethylated Quinazolin-4(3 H)-ones with Trifluoroacetic Acid as CF3 Source.
J Org Chem
; 83(9): 5104-5113, 2018 05 04.
Article
em En
| MEDLINE
| ID: mdl-29648821
ABSTRACT
A novel and convenient one-pot sequential cascade method for the preparation of 2-trifluoromethylquinazolin-4(3 H)-ones is described. Trifluoroacetic acid (TFA) was employed as inexpensive and readily available CF3 source, which in the presence of T3P was condensed with a variety of anthranilic acids and amines to provide the products in up to 75% yield. The protocol was proved to be robust on 80 g scale, and the synthetic versatility of the prepared quinazolinon-4-ones was demonstrated by derivatization to further useful building blocks.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinazolinas
/
Ácido Trifluoracético
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article