Trans 2,3-disubstituted-2,3-dihydro-5-hydroxybenzofurans as...

C - Chemistry – Metallurgy – 07 – D

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260/361, 260/327

C07D 307/79 (2006.01) C07D 307/80 (2006.01) C07D 409/06 (2006.01)

Patent

CA 2025478

90/VJC29 17969 TITLE OF THE INVENTION TRANS 2,3-DISUBSTITUTED-2,3-DIHYDRO-5-HYDROXY- BENZOFURANS AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS ABSTRACT OF THE DISCLOSURE The novel trans-2,3-disubstituted-2,3- dihydro-5-hydroxybenzofurans are described. The synthesis involves an intramolecular Michael addition to yield the thermodynamic trans isomer. The compounds were found to be inhibitors of 5-lipoxygenase, an enzyme crucial to the biosynthesis of leukotrienes and useful for the treatment of various inflammatory diseases.

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