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note
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3S requires C, 70.98; H, 5.36%.
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0011181186
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Ger. Offen. DE 3006277, 4 Sep 1980, 26 pp
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α-Bromoketones were prepared via Friedel-Crafts acylation of the appropriate arene followed by bromination of the resulting ketone according to the similar procedure described in the literature. See for example: (a) Giordano, C.; Casagrande, F. Ger. Offen. DE 3006277, 4 Sep 1980, 26 pp, Chem. Abstr. 94:30372; (b) Carter, J. S.; Rogier, D. J.; Graneto, M. J.; Seibert, K.; Koboldt, C. M.; Zhang, Y.; Talley, J. Bioorg. Med. Chem. Lett. 1999, 9, 1167-1170.; (c) Almansa, C.; de Arriba, A. F.; Cavalcanti, F. L.; Gomez, L. A.; Miralles, A.; Merlos, M.; Garcia-Rafanell, J.; Forn, J. J. Med. Chem. 2001, 44, 350-361.
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0033583468
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α-Bromoketones were prepared via Friedel-Crafts acylation of the appropriate arene followed by bromination of the resulting ketone according to the similar procedure described in the literature. See for example: (a) Giordano, C.; Casagrande, F. Ger. Offen. DE 3006277, 4 Sep 1980, 26 pp, Chem. Abstr. 94:30372; (b) Carter, J. S.; Rogier, D. J.; Graneto, M. J.; Seibert, K.; Koboldt, C. M.; Zhang, Y.; Talley, J. Bioorg. Med. Chem. Lett. 1999, 9, 1167-1170.; (c) Almansa, C.; de Arriba, A. F.; Cavalcanti, F. L.; Gomez, L. A.; Miralles, A.; Merlos, M.; Garcia-Rafanell, J.; Forn, J. J. Med. Chem. 2001, 44, 350-361.
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33
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0035253874
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α-Bromoketones were prepared via Friedel-Crafts acylation of the appropriate arene followed by bromination of the resulting ketone according to the similar procedure described in the literature. See for example: (a) Giordano, C.; Casagrande, F. Ger. Offen. DE 3006277, 4 Sep 1980, 26 pp, Chem. Abstr. 94:30372; (b) Carter, J. S.; Rogier, D. J.; Graneto, M. J.; Seibert, K.; Koboldt, C. M.; Zhang, Y.; Talley, J. Bioorg. Med. Chem. Lett. 1999, 9, 1167-1170.; (c) Almansa, C.; de Arriba, A. F.; Cavalcanti, F. L.; Gomez, L. A.; Miralles, A.; Merlos, M.; Garcia-Rafanell, J.; Forn, J. J. Med. Chem. 2001, 44, 350-361.
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0011190334
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Mechanistically, the reaction proceeds via in situ generation of the phenacyl ester followed by an intramolecular aldol-type condensation leading to the formation of the corresponding furanone, which subsequently can react with molecular oxygen to yield the product. See for example: Ref. 18
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Mechanistically, the reaction proceeds via in situ generation of the phenacyl ester followed by an intramolecular aldol-type condensation leading to the formation of the corresponding furanone, which subsequently can react with molecular oxygen to yield the product. See for example: Ref. 18 .
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24 (% inhibition was recorded @10 μM concentration of the drug). Selective inhibition of COX-2 over COX-1 is beneficial for the treatment of inflammatory diseases with reduced ulcerogenic side effects. See: Jackson, L. M.; Hawkey, C. J. Expert Opin. Invest. Drugs 1999, 8, 963-971.
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