Process for the preparation of quinargine

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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546170, C07D21536, C07D21538

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active

059144041

ABSTRACT:
The present invention is concerned with a novel process for the manufacture of quinargine ##STR1## (N-(2-quinolylcarbonyl)-asparagine) based on the reaction of the succinimide ester ##STR2## with asparagine or asparagine salts in an aqueous reaction medium at a neutral pH value.

REFERENCES:
patent: 5480887 (1996-01-01), Hornback et al.
G.W. Anderson, et al., The Use of Esters of N-Hydroxysuccinimide in Peptide Synthesis, J. Am. Chem. Soc., vol. 86, pp. 1839-1842 (1964).
J.W. Davis, Studies with Quinolines. I. Synthesis of Quinaldic Acid and Some of Its Amide Derivatives, J. Org. Chem., vol. 24, pp. 1691-1694 (1959).
P. Stelzel, Methoden der organischen Chemie; Synthese von Peptiden, vol. 15, part 2, pp. 214-259 (1974).
G. Wendelberger, Methoden der organischen Chemie; Synthese von Peptiden, vol. 15, part 2, pp. 130-169 (1974).
Chemical Abstracts 120:245780, 1993.
Chemical Abstracts 115:183974, 1991.

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