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Summary:NEW MATERIAL:A compound shown by the formula I . USE:An analgesic. PREPARATION:For example, a compound shown by the formula H-Arg(NO2)- OBzl.2TosOH (Bzl is benzyl; Tos is paratoluenesulfonyl) is dissolved in DMF, reacted with a compound shown by the formula Z(OMe)-Tyr(Bzl)-OTGCP(Me is methyl; TCP is 2,4,5-trichlorophenyl) in the presence of a tertiary amine to give a compound shown by the formula II. This compound is then reacted with trifluoroacetic acid, and reacted with a compound shown by the formula Boc- Arg(NO2)-OH(Boc is t-butyloxycarbonyl) to give a compound shown by the formula III. This compound is further reacted with a compound shown by the formula Z(OMe)-Tyr(Bzl)-OTCP, treated with TFA, and reacted with Boc-Arg (NO2)-OH, ethylchoroformate, etc., to give a compound shown by the formula IV. Finally this compound is reacted with a compound shown by the formula Z (OMe)-Tyr(Bzl)-OTCP, and the protecting group is removed, to give a compound shown by the formula I .
Bibliography:Application Number: JP19830229557