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2005
Triazole derivatives
Triazole derivatives
R 0280
Syntheses of 1-(4-Methylsulfonylphenyl)-5-aryl-1,2,3-triazoles and 1-(4-Amino— Biaryltriazoles (VI) and (XII) are synthe28- 139 sulfonylphenyl)-5-aryl-1,2,3-triazoles.
sized as possible COX-2 inhibitors. Some reaction steps according to literature methods
are slightly modified to start the reaction or to improve the reaction yields. For example,
potassium permanganate oxidation of (V) in an acetone solution affords the desired
product (VI) only in low yield. However, this compound can be obtained in moderate
to good yield using potassium permanganate in a two-phase system in the presence of
a phase-transfer catalyst. Because the cycloaddition of diazomethane (IV) with sulfonamide-group-bearing imino compound fails, the synthesis of triazole (XII) involves the
protection of the amino group as dibenzylamine, cf. (IX). — (DAHA, F. J.;
MATLOUBI, H.; TABATABI, S. A.; SHAFII, B.; SHAFIEE*, A.; J. Heterocycl.
Chem. 42 (2005) 1, 33-37; Pharm. Sci. Res. Cent., Tehran Univ. Med. Sci., Tehran,
Iran; Eng.) — H. Hoennerscheid
2005
Triazole derivatives
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