NEW MATERIAL:The compound of formula I [X is group of formula II or formula III; n is 1 or 0; Y is group of formula IV, formula V (R1 is H or alkyl; m is 1W3; X is H or halogen), etc.] and its salt.
USE: An analgesic and central nervous suppressing agent. It has weak agonistic activity to the opiate receptor, and is useful as an analgesic having low narcotic property.
PROCESS: The compound of formula I can be prepared from a peptide and the amine compound corresponding to the amine segment denoted by Y in the formula I , by conventional condensation process for peptide synthesis. As an alternative method, the objective compound can be obtained by using the amine compounds as starting substances, and extending the amino acid residues successively by the conventional condensation process for peptide synthesis. The third process for the preparation of the objective compound is condensation of the amino acids or peptide derivatives of the amine compounds with amino acids or peptides by conventional condensation process for peptide synthesis.
SASAJIMA KIKUO
KAI HIROYUKI
SUWA KAZUYUKI
KOGA YOSHIHIKO
HARA NOBUYUKI