Synthesis of homochiral dihydroxy-4-nitroisoxazolines via one-pot asymmetric dihydroxylation-reduction.

Herein we report a one-pot procedure to prepare a family of homochiral dihydroxy-4-nitroisoxazolines 3. This new methodology affords the title compounds in good yields, excellent enantiopurity, and without the use of chromatography.

Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.

A number of naphthofuranones were synthesized and tested for COX-1 and COX-2 inhibition. Few of them were identified as selective COX-2 inhibitors. Structure-activity relationship studies within the series are discussed.