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KMID : 0370220040480020135
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Yakhak Hoeji
2004 Volume.48 No. 2 p.135 ~ p.140
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Synthesis of Potential COX-2 Inhibitory 1,5-Diarylhydantoin Derivatives
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권순경/Kwon SK
박해선/Park HS
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Abstract
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Fer the development of new COX-2 inhibitors, 1,5-diarylhydantoins 5a-5c and 1,5- diaryl-2-thiohydantoin 6a-6c were synthesized from commercially available phenylacetic acids th rough esterifcation, bromination, C-N bond formation and cyclization. Esters 2a-c were efficiently synthesized from the starting materials la- c by reflux(ins in absolute methanol for 3 hours with catalytic concentrated sulfuric acid. Bromination of 2a-c was carried out with use of N-bomo-succinimide at rt in dichloromethane. The bromine of 3a~c was substituted with aniline in ethanol or N,N- dimethylformamide to provide 4a~c. Hydantoins and 2-thiohydantoins were synthesized from 4a~c by treatment of potassium isocyanate or potassium thiocyanate in dil- ethanol with triethylamine.
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