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An optimized, easy to scale-up synthetic route for a tetrahydrothiophene linker useful for the preparation of C-terminal peptide α-ketoacids is described. Loading this linker on the solid support allows preparation of side-chain unprotected peptide cyanosulfurylides, which are easily oxidized to generate the corresponding C-terminal peptide α-ketoacids. The peptide α-ketoacids serve as protease inhibitors...
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