反应详情

A solution of 1.22 g (3.92 mmoles) of ethyl 1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate, 0.86 g (7.85 mmoles) of 3hydroxyazetidine hydrochloride, 2 g (19.8 mmoles) of triethylamine and 20 ml of dimethyl sulphoxide (DMSO) is heated for 4 hours at 80° C. The solution is allowed to cool and is added to a mixture of ice and water, giving a precipitate which is filtered and washed with water. The solid is dried under vacuum yielding 1.40 g (97%) of ethyl 1-cyclopropyl-6,8-difluoro-7-(3-hydroxy-1-azetidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylate melting at 260°-270° C.

1. temperatureto cool
2. customgiving a precipitate which
3. filtrationis filtered
4. washwashed with water
5. customThe solid is dried under vacuum