One-Pot Synthesis of Trifluoromethylated Quinazolin-4(3H)-ones with Trifluoroacetic Acid as CF₃ Source

Sofia Almeida, Roger Marti, Ennio Vanoli, Stefan Abele and Simone Tortoioli*

*Chemical Development, Idorsia Pharmaceuticals Ltd., Hegenheimermattweg 91, 4123 Allschwil, Switzerland, Email: simone.tortoioliidorsia.com

S. Almeida, R. Marti, E. Vanoli, S. Abele, S. Tortoioli, J. Org. Chem., 2018, 83, 5104-5113.

DOI: 10.1021/acs.joc.8b00389

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Abstract

In a convenient one-pot sequential cascade synthesis of 2-trifluoromethylquinazolin-4(3H)-ones, trifluoroacetic acid serves as inexpensive and readily available CF₃ source. Condensation of anthranilic acids with TFA in the presence of T3P followed by condensation with amines provides the desired products in good yield.

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T3P

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Key Words

quinazolin-4(3H)-ones

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ID: J42-Y2018