| 摘要 |
<p>PURPOSE: A manufacturing method for a peptide is provided to minimize a differentiation of His2 and Ser4 in a hydrolysis step, to purify in a commercial size, and to obtain with a good yield rate. CONSTITUTION: A peptide of the formula (I):5-oxo-Pro-R1-Trp-Ser-R2-R3-R4-Arg-Pro-R6, wherein R1 represents His, Tyr, Trp or p-NH2-Phe, R2 represents Tyr or Phe, R3 represents an optionally substituted Gly or an optionally substituted alpha-D-amino acid residue, R4 represents Leu, Ile or Nle, R6 represents (1) Gly-NH-R7, wherein R7 represents a hydrogen atom or an alkyl group which may optionally be substituted with a hydroxyl group, or (2) NH-R8, wherein R8 represents a hydrogen atom, an alkyl group which may optionally be substituted with a hydroxyl group or an ureido group (-NH-CO-NH2), is produced advantageously in an industrial scale by reacting a peptide of the formula (II):5-oxo-Pro-R1-Trp-Ser-R2-R3-OH, wherein R1, R2 and R3 have the same meanings as defined above or its salts, with a peptide of the formula (III):H-R4-R5-Pro-R6, wherein R4 and R6 have the same meaning as defined above and R5 represents Arg which has been protected or its salts, to produce a peptide of the formula (I'):5-oxo-Pro-R1-Trp-Ser-R2-R3-R4-R5-Pro-R6, wherein R1, R2, R3, R4, R5 and R6 have the same meanings as defined above or its salt, and then subjecting thus obtained peptide (I') to a de-protecting group reaction.</p> |
