Dimethyl Sulfoxide → Ethyl 7-[3-[(acetylamino)methyl]-1-azetidinyl]-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate

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Reaction Steps

A solution of 1.0 g (3.2 mmoles) of ethyl 1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate, 1.05 g (6.4 mmoles) of 3-acetamido-methylazetidine hydrochloride, 1.6 g (16 mmoles) of triethylamine and 20 ml of DMSO is heated to 80° C. for 4 hours. It is allowed to cool, poured onto a mixture of ice and water giving a precipitate which is filtered and washed with water. The solid is dried under vacuum yielding 0.93 g (69%) of ethyl 7-(3-acetamidomethyl-1-azetidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate melting at 170°-190° C.

Provenance & Evidence