Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoro-methyl)phenyl]-1,2-dihydroquinoline-3-carboxamide

摘要

Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl) -phenyl]-1,2-dihydroquinoline-3-carboxamide, having a deuterium enrichment in the amide-N methyl group of at least 70%; or a salt thereof with a pharmaceutically acceptable organic or inorganic cation; and a method of preparing said compounds. The compounds are useful in therapy, e.g. for the treatment of a malignant hyperproliferative disorder or an autoimmune disease.

主权项

1. A method of preparing a deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl)phenyl]-1,2-dihydroquinoline-3-carboxamide, or a pharmaceutically acceptable salt thereof, comprising
reacting a C1-C4 alkyl ester of 4-hydroxy-5-methoxy-1-methyl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid with deuterium-enriched N-methyl-p-trifluoromethylaniline, wherein the N-methyl group has a deuterium enrichment of at least 70%.