| 摘要 |
<p>PURPOSE:To obtain the titled compound having physiological activity efficiently, by reacting an N-carboxy-alpha,beta-dehydro-alpha-amino acid anhydride with an amino group-protecting agent, etc., and a nucleophilic substance successively. CONSTITUTION:A compound shown by formula I (R1 and R2 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-alpha-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-alpha-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 (X1 is acyl type protecting group; Y2 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 (Y3 is alkyl; AA1 is alpha-amino acid residue) as the acryl type protecting agent as the component A and an alpha-amino acid alkyl ester as the component B.</p> |
