Isopropanol → alpha-Formyl aspartic acid benzyl amide

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Reaction Steps

The yellowish oil of example 1, dissolved in 100 ml isopropanol, is compounded with 14 ml (100 mmol) triethylamine and compounded with 10 ml (100 mmol) benzylamine. The mixture is heated for 3 h to 50° C. After removal of the isopropanol in a vacuum the residue is taken up in 100 ml 1 N HCl, agitated 1 h and then extracted several times with ethyl acetate. The saturated organic phases are dried over magnesium sulfate and after filtration the solvent is removed in a vacuum. 20 g (80 mmol) 80% of a slightly yellowish solid is obtained.

Provenance & Evidence