Preparation of 2-trifluoromethyl cinchoninic acids

Details Preparation of 2-trifluoromethyl cinchoninic acids Preparation of 2-trifluoromethyl cinchoninic acids

C - Chemistry, Metallurgy

07

D

260/289

C07D 215/50 (2006.01)

Patent

CA 1133489

11837 PREPARATION OF 2-TRIFLUOROMETHYL CINCHONINIC ACIDS ABSTRACT OF THE DISCLOSURE 2-Trifluoromethyl cinchoninic acids can be pre- pared in high yields by reaction of an alkali metal 2-amino- phenylglyoxylate and 1,1,1-trifluoroacetone in the presence of a weak acid and a metal salt of a weak acid. Preferably reaction is effected by first hydrolyzing isatin, or a sub- stituted isatin, in the presence of an alkali metal hydroxide to produce the alkali metal 2-aminophenylglyoxylate, and then reacting this intermediate product with 1,1,1-trifluoro- acetone without isolating it from the reaction medium.

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