PREPARATION OF OLIGOPEPTIDE

摘要

PURPOSE:To prepare the titled compound useful as an analgesic for warm- blooded animals such as man, from a specific tripeptide and a dipeptide, etc., by carrying out the condensation reaction of X-Arg without protecting the guanidyl group of Arg. CONSTITUTION:A pentapeptide of formula B-X-Arg-Aly-Leu is prepared by condensing the tripeptide of formula Arg-Aly-Leu-Y[Y is OH or NR<1>R<2> (R<1> and R<2> are H or alkyl)]and the dipeptide of formula B-X (B is Phe or alkyl- Phe; X is Met, Met-sulfoxide or Leu) between X and Arg without protecting the guanidyl group of Arg. The pentapeptide is condensed with the tripeptide of formula Tyr-A-Gly (A is Gly or Ala) to obtain the oligopeptide of formula. Dose: 0.01-100mg/kg/day by oral or parenteral administration.