Improved Synthesis of a Smad3 Phosphorylation Inhibitor Lingzhifuran A via Condensation Reaction

Abstract
A facile and high-efficient synthesis of lingzhifuran A, a Smad3 phosphorylation inhibitor isolated from Ganoderma lucidum, was developed from commercially available dibenzo[b,d]furan. The crucial step of this strategy was achieved via condensation reaction using key intermediate 8-hydroxydibenzo[b,d]furan-4- carbaldehyde and commercially available (E)-2-methylbut-2-enal. By this strategy, lingzhifuran A was obtained in 5 steps with up to 57.6% yield.
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