| 摘要 |
Undecapeptides of the formula: L-pyroglutamyl - L - prolyl - L - seryl - L - lipyl - R1-L - alanyl - L - phenylalanyl - R2 - glycyl - L-leucyl - L - methionine amide in which R1 is L - glutaminyl, L - glutamyl, L - asparaginyl, or glycyl, R2 is L-isoleucyl, L-leucyl, or L-valyl and R1 may be L-aspartyl when R2 is L-leucyl or L-valyl are prepared by condensing the individual amino acids to form tri- and tetra-peptides which are in turn condensed with each other. In the process a methyl ester of an amino acid or a peptide may be hydrolysed to the free acid by means of a proteolytic enzyme e.g. trypsine or chymotrypsine. The following intermediates are prepared: - Cbo - Glu(OtBu) - Ala - PheOMe; H - Glu (Ot - Bu) - Ala - Phe OMe; H - Pyroglu - Pro-Ser - Lys(BOC)OH; H - Pyroglu - Pro - Ser-Lys(BOC) - Glu(OtBu) - Ala - PheOMe and its free acid (by enzymic hydrolysis) and H-Pyroglu-Pro - Ser - Lys(BOC) - Glu(OtBu) - Ala - Phe-Ileu - Gly - Leu - MetNH2. Cbo - Asp(NH2)-Ala - Phe - OMe; H - Asp(NH2) - Ala - Phe-OMe, HCl, H Pyroglu - Pro - Ser - Lys(BOC)-Asp(NH2) - Ala - Phe - OMe and its free acid. Cbo - Lys (BOC) - Asp(NH2) - PheOMe; Cbo-Pro - Ser - Lys (BOC) - Asp(NH2) - Ala - Phe-OMe; H - Pyroglu - Pro - Ser - Lys (BOC)-Asp (NH2) - Ala - Phe - Ileu - Gly - Leu-MetNH2; Cbo - Asp(Ot - Bu) - Ala - Phe-Ome; H - Pyroglu - Pro - Ser - Lys (OtBu)-Asp(OtBu) - Ala - Phe - OMe; BOC - Gly - Ala-Phe -OMe and its hydrazide; BOC - Gly-Ala - Phe - Ileu - Gly - Leu - Met - NH,; H-Gly - Ala - Phe - Ileu - Gly - Leu - MetNH2; BOC - Gly - Ala - Phe - Leu - Gly - Leu - Met NH2 and H-Gly-Ala-Phe-OMe, HCl. |
