Production of specific substance containing alpha,beta-dehydro-alpha-amino acid residue

Abstract

PURPOSE: To obtain the titled compound having physiological activity efficiently, by reacting an N-carboxy-α,β-dehydro-α-amino acid anhydride with an amino group-protecting agent, etc., and a nucleophilic substance successively. CONSTITUTION: A compound shown by formula I (R 1 and R 2 are carboxyl, alkyl or aryl which may be replaced, respectively but are not H at the same time) is reacted with (A) a substance consisting of an amino group-protecting agent or an N-protecting-α-amino acid (halide) in the presence of a base or a condensation agent and the base and then a prepared compound shown by formula II (X is amino group-protecting group or N-protecting-α-amino acid residue) is reacted with (B) a nucleophilic substance in the presence of the base to give the aimed substance. For example, a compound shown by formula III (X 1 is acyl type protecting group; Y 2 is water) is obtained by using an acyl type protecting agent as the component A and water as the component B and a compound shown by formula IV (Y 3 is alkyl; AA 1 is α-amino acid residue) as the acryl type protecting agent as the component A and an α-amino acid alkyl ester as the component B. COPYRIGHT: (C)1988,JPO&Japio

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Cited By (2)

    Publication numberPublication dateAssigneeTitle
    US-6762277-B2July 13, 2004Jsr CorporationMethod of manufacturing N-carboxyamino acid anhydride and polyamino acid
    WO-9622970-A1August 01, 1996Bayer AktiengesellschaftDerives d'amide d'aminoacide et leur utilisation comme pesticides