Synthesis of Ethyl 6,7-Difluoro-4-hydroxy-2-[(methoxymethyl)thio]-quinoline-3-carboxylate

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Synthesis of Ethyl 6,7-Difluoro-4-hydroxy-2-[(methoxymethyl)thio]-quinoline-3-carboxylate

Published 2004 · Cheng Chun

Chinese Journal of Pharmaceuticals

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Abstract

Ethyl 6,7-difluoro-4-hydroxy-2-[(methoxymethyl)thio]quinoline- 3-carboxylate, a key intermediate ofprulifloxacin, was synthesized by treatment of 3,4-difluoroaniline with carbon disulfide in the presence of triethylamine andthen reacted with ethyl chloroformate to give 3,4-difluorophenylisothiocyanate, which reacted successively with diethylmalonate in the presence of KOH and chloromethyl methyl ether and then cyclization with an overall yield of 85.7%.

Study Snapshot

Ethyl 6,7-difluoro-4-hydroxy-2-[(methoxymethyl)thio]-quinoline-3-carboxylate, a key intermediate in prulifloxacin, was synthesized with 85.7% overall yield using a novel process.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Synthesis of Ethyl 6,7-Difluoro-4-hydroxy-2-[(methoxymethyl)thio]-quinoline-3-carboxylate

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