Synthesis of a derivative of GRF and intermediate peptides.

摘要

A process for the manufacture of a polypeptide (I) having the formula:which comprises steps of:
(a) coupling, successively and in the order of the sequence of the polypeptide (I), the four protected fragments A, B, C and D or five protected fragments A, B, C, E and F,said fragment A by the formula, Leu-Gln-Asp-Ile-Met-Ser-Arg-NH₂said fragment B by the formula, Gln-Leu-Ser-Ala-Arg-Lys-Leusaid fragment C by the formula, Arg-Lys-Val-Leu-Glysaid fragment D by the formula, Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyrsaid fragment E by the formula, Ile-Phe-Thr-Asn-Ser-Tyr and said fragment F by the formula, Tyr-Ala-Asp-Ala being represented, respectively, and(b) eliminating, at the end of sequence, all the protecting groups to provide the polypeptide (I) which is active on the stimulation of the release of the growth hormone and thus is very useful as medicine for treatment of growth hormone deficiency disease and the like.