• YAKHAK HOEJI
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• v.59 no.2
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• pp.66-69
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• 2015

A concise synthesis of flurbiprofen, a member of the non-steroidal anti-inflammatory 2-arylpropionic acids, has been accomplished. The key feature of this synthesis involves successive palladium-catalyzed cross coupling reactions. In particular, a 2-arylacylate intermediate, which easily converted to the key 2-arylpropionic acid scaffold, was afforded by a versatile palladium-catalyzed cross coupling reaction between diazopropanate and bisphenylboronic acid. This synthetic procedure would facilitate synthesis of the flurbiprofen and anti-inflammatory 2-arylpropionic acid derivatives.

• YAKHAK HOEJI
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• v.23 no.2
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• pp.119-124
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• 1979

Eight derivatives of arylpropionic acid, arylcarbonylpropicnic acid, and arylhydroxybutyric acid were synthesized and their structures were elucidated on the basis of elemental analysis and spectral data. Also their antiinflammatory activities were evaluated by the method of the inhibitory effect on the carrageenin-induced rat paw edema and compared with phenylbutazone. Compound (I) exhibited 59% edema inhibition vs control when 100 mg/kg, was orally administered, whereas phenylbutazone showed 57.8% for 50mg/kg.

• Archives of Pharmacal Research
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• v.10 no.1
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• pp.25-28
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• 1987

(+)-Ketoprofen was obtained form resolution with (S) (+)-2-amino-1-butanol and its absolute configuration was determined to be (S) by chemical correlation with (S) (+)-ethyl hydratropate using Beckmann rearrangement as a key step.