Investigation on the reactions of the 4-tosylamino derivative of 5,7-dichlorokynurenic acid with glycine, glycolic acid and thioglycolic acid

CHED 420

Alfred C. Nichols, anichols@jsu.edu, Nagarajan Vasumathi, nvasumat@jsu.edu, and Stephen E Craig, jsu8156j@jsu.edu. Department of Physical and Earth Sciences, Jacksonville State University, 700 Pelham Road North, Jacksonville, AL 36265
The 4-tosylamino derivative of 5,7-dichlorokynurenic acid was treated first with triphosgene and then with glycine in an attempt to produce the corresponding [({[5,7-dichloro-2-(ethoxycarbonyl)quinolin-4-yl]amino}carbonyl)amino]acetic acid derivative. The reaction led to the formation of an unexpected detosylated product that was difficult to purify. The impure product was refluxed with thionyl chloride in absolute ethanol and produced a product which was identified by NMR and elemental analysis as the 4-(ethyl N-carbamate) derivative of 5,7-dichlorokynurenate ethyl ester. Detosylation was also observed when either glycolic acid or thioglycolic acid was substituted for glycine.