1-methyl-2-(trifluoromethyl)-1H-1,3-benzodiazole-5-carboxylic acid synthesis
- Product Name:1-methyl-2-(trifluoromethyl)-1H-1,3-benzodiazole-5-carboxylic acid
- CAS Number:1094264-29-5
- Molecular formula:C10H7F3N2O2
- Molecular Weight:244.17
66315-15-9
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Yield:1094264-29-5 60%
Reaction Conditions:
with hydrogenchloride in water; for 24 h;Inert atmosphere;Reflux;
Steps:
5.1.2. General procedure for the synthesis of compounds 7e-7g, 7n
General procedure: The appropriate 1,2-phenylenediamine (9a, 9b, 12, 14, 0.0313 mol), 1.6 eq of CF3CO2H and one drop of concentrated HCl were heated under reflux in a N2 atmosphere for 24 h. After completion of the reaction, the cooled mixture was neutralized with saturated NaHCO3 solution and the crude product was extracted with ethyl acetate. The combined organic extracts were washed with water, dried with Na2SO4 and the solvent was removed under vacuum. The residue was dissolved in chloroform, filtered through Al2O3 neutral type and concentrated under vacuum to obtain the corresponding benzimidazole.
References:
Hernández-Covarrubias, Carlos;Vilchis-Reyes, Miguel A.;Yépez-Mulia, Lilian;Sánchez-Díaz, Remedios;Navarrete-Vázquez, Gabriel;Hernández-Campos, Alicia;Castillo, Rafael;Hernández-Luis, Francisco [European Journal of Medicinal Chemistry,2012,vol. 52,p. 193 - 204] Location in patent:experimental part
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