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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:

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

DOI: 10.1021/acs.joc.8b00389 (free Supporting Information)


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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ID: J42-Y2018