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KMID : 0617220010120010003
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Duksung Bulletin Phamaceutical Sciences
2001 Volume.12 No. 1 p.3 ~ p.6
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Synthesis of Novel Methyl α-Anilinophenylacetate Derivatives for 1,5-Diphenylhydantoins
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Abstract
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For the development of new COX-2 inhibitor, novel key intermediates (2∼4) synthesized through esterification, bromination and α-substitution from phenylacetic acid. The methyl phenylacetate 2 was synthesized through reflux phenylacetic acid with sulfuric and methanol. The methyl α-bromophenylacetate 3 was produced through radical bromination using N-bromosuccinimide from 2. The optical amination to introduce anilino group was contolled under 80℃ in DME. The bromo intermediate was converted to the final methyl α-anilinophenylacetate 4 through reaction with aniline.
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KEYWORD
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