| 摘要 |
PURPOSE:To obtain the subject peptide for treating Alzheimer disease, schizophrenia, etc., containing a new tyrosine derivative in an amino acid sequence and useful as a therapeutic agent for learning disability caused by abnormality of central nervous system, neurosis, aging, etc., of neurocyte. CONSTITUTION:A compound of the formula Boc-Tyr (Dmp)-R3-Gly-OH (Boc is t-butyloxycarbonyl; Dmp is dimethylphosphinyl; R3 is Nle, Thr, etc.) is made to react with a compound of the formula H-Trp-R4-Asp(OBzl)-Phe- NH2.hydrochoride (R4 is Nle, etc.; Bzl is benzyl) in the presence of a condensation agent to afford the formula Boc-Tyr (Dmp)-R3-Gly-Trp-R4-Asp-Phe-NH2, which is then subjected to catalytic reduction using 10% palladium active carbon catalyst to provide the objective peptide having pharmacological activity, expressed by the formula (R1 is H, methyl, Boc, acetyl, etc.; R2 is Dmp, dimethylcarbamoyl, etc.) and containing a new tyrosine derivative in an amino acid sequence. |
