| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for producing a peptide having action as an antagonist of gonadotropic hormone-releasing hormone (LH-RH) on an industrial scale. SOLUTION: A peptide of formula II 5-oxo-Pro-R<1> -Trp-Ser-R<2> -R<3> -OH [in the formula, R<1> is His, Tyr, Trp or p-NH2 -Phe; R<2> is Tyr or Phe; R<3> is Gly or anα-D-amino acid residue which may contain a substituent group, respectively] or its salt is reacted with a peptide of formula III H-R<4> -R<5> -Pro-R<6> [in the formula, R<4> is Leu, Ile or Nle; R<5> is a protected Arg; R<6> is a group of the formula Gly-NH-R<7> (in the formula, R<7> is a hydrogen atom or an alkyl which may contain a hydroxyl group) or a group of the formula NH-R<8> (in the formula, R<8> is a hydrogen atom or an alkyl group or a ureido group (-NH-CO-NH2 ) which may contain a hydroxyl group, respectively)] or its salt and the prepared peptide (I') is subjected to a deprotecting reaction to give a peptide of formula I 5-oxo-Pro-R<1> -Trp-Ser-R<2> -R<3> -R<4> -Arg-Pro-R<6> or its salt. In the formulas, the following abbreviations are used. Gly: glycine, Leu: leucine, Ile: isoleucine, Ser: serine, Arg: arginine, Phe: phenylalanine, Tyr: tyrosine, His: histidine, Trp: tryptophan, Pro: proline, Nle: norleucine. |
