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One-pot synthesis of trifluoromethylated quinazolin-4(3H)-ones with trifluoroacetic acid as CF3 source
Almeida, Sofia; Marti, Roger; Vanoli, Ennio; Abele, Stefan; Tortoioli, Simone
2018
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Résumé

A novel and convenient one-pot sequential cascade method for the preparation of 2-trifluoromethylquinazolin-4(3H)-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.

Détails

Titre
One-pot synthesis of trifluoromethylated quinazolin-4(3H)-ones with trifluoroacetic acid as CF3 source
Auteur(s)/ trice(s)
Almeida, Sofia (School of Engineering and Architecture (HEIA-FR), HES-SO University of Applied Sciences Western Switzerland ; Chemical Development, Idorsia Pharmaceuticals Ltd., Hegenheimermattweg 91, 4123 Allschwil, Switzerland)
Marti, Roger (School of Engineering and Architecture (HEIA-FR), HES-SO University of Applied Sciences Western Switzerland)
Vanoli, Ennio (School of Engineering and Architecture (HEIA-FR), HES-SO University of Applied Sciences Western Switzerland)
Abele, Stefan (Chemical Development, Idorsia Pharmaceuticals Ltd., Hegenheimermattweg 91, 4123 Allschwil, Switzerland)
Tortoioli, Simone (Chemical Development, Idorsia Pharmaceuticals Ltd., Hegenheimermattweg 91, 4123 Allschwil, Switzerland)
Date
2018-04
Publié dans
The Journal of Organic Chemistry (JOC)
Volume
2018, 83, 9, pp. 5104-5113
Pagination & équivalents
10 p.
DOI
https://doi.org/10.1021/acs.joc.8b00389
ISSN
0022-3263
Mots-clés (libres)
Trifluoromethylated Quinazolin-4(3H)-ones ; Trifluoroacetic Acid (TFA) ; CF3
Type d'article
scientifique
Domaine
Ingénierie et Architecture
Ecole
HEIA-FR
Institut
ChemTech - Institut des technologies chimiques
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