Preparation of Pseudo-Peptide Building Blocks with retro-Thioamide Bond Mediated via Thiocarbamoyl Meldrum's Acid

[摘要]：An easy and efficient synthesis of pseudo-tripeptide containing a thiomalonamide moiety was developed. Isothiocyanate derivatives of amino acids react smoothly with 2,2-dimethyl-1,3-dioxane-4,6-dione (Meldrum's acid) to yield new thiocarbamoyl derivatives of Meldrum's acids. Thermal decomposition of these new derivatives leads to thiocarbamoyl ketenes, which acylate amino acid esters to give pseudo-tripeptides.

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