Chloroform → ethyl 5-amino-7-fluoro-1-[2-(S)-fluoro-1-(R)-cyclopropyl]-1,4-dihydro-8-methoxy-4-oxoquinoline-3-carboxylate

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Reaction Steps

Ethyl 7-fluoro-1-[2-(S)-fluoro-1-(R)-cyclopropyl]-1,4-dihydro-8-methoxy-5-nitro-4-oxoquinoline-3-carboxylate (3.71 g, 10.1 mmol) was dissolved in acetonitrile (50 ml), and after adding a 5% palladium carbon catalyst (water content: 50%, 1.5 g) thereto, it was stirred at room temperature for 20 hours under a hydrogen atmosphere at atmospheric pressure. After removing the catalyst by filtering (methanol washing), the filtrate was concentrated under a reduced pressure, the residue obtained was applied to a silica gel chromatography, and 2.68 g (79%) of the title compound was obtained as a yellow amorphous substance from a chloroform:methanol=30:1 eluate.

Provenance & Evidence