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2005
Pyrazole derivatives
R 0180
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: A Novel Class of Potent, Selective
(COX-2) Inhibitors. — Reaction of Weinreb amides (I) with Grig16- 109 Cyclooxygenase-2
nard reagent (II) afford intermediates (III) in good yield. The use of an excess of Oxone
promotes a one-pot deprotection, oxidation, and cyclization to give pyrazoles (V)
directly from (III). The pyrazoles are evaluated for their ability to inhibit the COX-1
and COX-2 isoforms in human whole blood. In general, lipophilic or electron-rich substituents are preferred at the phenyl ring over electron deficient ones. Pyrazole derivative (Vb) is identified as a highly selective and potent COX-2 inhibitor. —
(RANATUNGE*, R. R.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 24, 6049-6052;
NitroMed, Inc., Lexington, MA 02421, USA; Eng.) — H. Hoennerscheid
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