Abstract
AbstractThe syntheses of 6‐fluoro‐7‐piperazin‐1‐yl‐9‐cyclopropyl (or 9‐p‐fluorophenyl)‐2,3,4,9‐tetrahydroisothiazolo[5,4‐b]quinoline‐3,4‐diones as well as novel synthesis of isothiazolo‐3(2H)‐one system are described. Key steps include the regiospecific displacement of a sulfinyl group and the amination of the resultant mercapto derivative followed by an intramolecular nucleophilic displacement cyclization reaction to generate the novel 2,3,4,9‐tetrahydroisothiazolo[5,4‐b]quinoline‐3,4‐dione nucleus.
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