Fmoc Rink linker is a widely used peptide-resin linker in the solid-phase synthesis of peptide-amides. This paper describes an improved and practical eight-step synthetic approach for this compound in a 50% overall yield, using p-hydroxybenzaldehyde as the starting material. The procedure is operationally simple and amenable to scale-up synthesis.
A practical three-step synthetic approach to gimeracil in a 68% overall yield is described, using 2,4-dimethoxypyridine as the starting material with 3,5-dichloro-2,4-dimethoxypyridine and 3,5-dichloro-2,4-dihydroxypyridine as intermediates. The advantages of this procedure include short reaction steps, simple operation and good yield.
A practical eight-step synthesis of a key intermediate of beraprost is described. The tricyclic cyclopent[ b]benzofuran core can be prepared from 2,6-dibromo-4-chlorophenol. The butyric side chain is introduced by ortho-selective metal–halogen exchange and subsequent coupling with 4-(benzyloxy)butanal. The procedure is operationally simple and amenable to scale-up synthesis.
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