abstract |
The present invention relates to a process for the preparation of known anti-inflammatory N-aryl anthranilic acids and derivatives thereof, such as esters, amides and hydroxamic acid esters. In the general formula (I), the substituents have a wide variety, for example, R1 is hydrogen, alkyl, alkoxy or aryl; R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9 and R 10 are, for example, independently selected from halogen, alkyl, aryl, heterocyclic, haloalkyl, -CN, - (O) m - (CH 2) n R11 or - [N (H)] m- (CH2) n-R11 is a group or any two substituents on any of the adjacent ring carbon atoms of R 2, R 3, R 4, R 5, R 6, R 7, R 8, R for example, aryl, heterocyclic or cycloalkyl, or R 1 and R 6 together with the nitrogen to which R 1 is attached, and, for example, together with the carbon atom to which R 6 is attached may form a 5- or 6-membered aromatic or dihydroaromatic ring, Z is -COOH, - COOM, -COOR15, -C (O) N (R16) R17, -C (O) N (R18) OR19, -NO2 or -CN. The compound of formula (I) is prepared in a variety of ways, for example by reacting a compound of formula (A) with a compound of formula (B), optionally in a solvent and in the presence of a base of from 1 to 10 molar equivalents. HE |