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179246-09-4

4(3H)-Quinazolinone, 6-(trifluoromethoxy)- synthesis

1synthesis methods
Benzoic acid, 2-aMino-5-(trifluoroMethoxy)-, hydrochloride

746671-63-6
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3473-63-0 Synthesis
Formamidine acetate

3473-63-0
497 suppliers
$5.00/25g

4(3H)-Quinazolinone, 6-(trifluoromethoxy)-

179246-09-4
15 suppliers
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Yield:179246-09-4 82%

Reaction Conditions:

in 2-ethoxy-ethanol; for 2 h;Heating / reflux;

Steps:

D4.4

A mixture of 2-amino-5-trifluoromethoxy-benzoic acid, HCl salt (1.52 g, 5.91 mMol), and formamidine acetate (1.84 g, 17.73 mMol) in 2-ethoxyethanol (20 mL) was heated at reflux for 2 hours. Analysis by LC/MS showed that the reaction was complete, so the mixture was concentrated in-vacuo, and the residue was purified over silica gel, eluting with 50% ethyl acetate/heptane-100% ethyl acetate, to yield 1.1 g of white solids as product. MS (ES+)=231 (M+H)+. Yield=82%.

References:

US2005/54626,2005,A1 Location in patent:Page/Page column 39