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A flexible approach to ethyl (3R, 4S)-N-Boc-4-amino-3-hy-droxy-5-phenylpentanoate (N-Boc-AHPPA-OEt), the γ-ammino-β-hydroxy acid moiety of hapalosin is described. The syntheticmethod features a ring-opening ethanolysis of an activated N-Boc-lactam, which is obtained via a diastereoselective reductive-alkylation or (R)-malimide derivative. The flexibility of themethod resides in the introduction of the alkyl side chain byGrignard reagent addition.
A flexible approach to ethyl (3R, 4S) -N-Boc-4-amino-3-hy-droxy-5- phenylpentanoate (N-Boc-AHPPA- OEt), the γ- ammino- β-hydroxy acid moiety of hapalin is described. The syntheticmethod features a ring-opening ethanolysis of an activated N-Boc-lactam, which is obtained via a diastereoselective reductive-alkylation or (R) -malimide derivative. The flexibility of themethod resides in the introduction of the alkyl side chain byGrignard reagent addition.