1-Cyclopropyl-3-ethoxycarbonyl-7,8,9-trifluoro-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine → 8-(3-Amino-1-azetidinyl)-1-cyclopropyl-3-ethoxycarbonyl-7,9-difluoro-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine

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Reaction Steps

8-(3-Amino-1-azetidinyl)-1-cyclopropyl-3-ethoxycarbonyl-7,9-difluoro-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine was prepared under the conditions of Example 2, but starting with 1.3 g of 1-cyclopropyl-3-ethoxycarbonyl-7,8,9-trifluoro-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine and 1.32 g of 3-aminoazetidine dimethanesulphonate. After recrystallization in 50 cm3 of ethanol, 0.8 g of 8-(3-amino-1-azetidinyl)-1-cyclopropyl-3-ethoxycarbonyl-7,9-difluoro-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine is obtained in the form of a yellow solid, melting point 236°-238° C.

Provenance & Evidence