Synthesis of hgrf (somatocrinin) in liquid phase

C - Chemistry – Metallurgy – 07 – K

Patent

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530/5.04, 530/7.

C07K 5/04 (2006.01) C07K 7/04 (2006.01) C07K 14/60 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1254349

ABSTRACT OF THE DISCLOSURE A process for the synthesis, in liquid phase and by fragments, of hGRF 1-44 and hGRF 1-40. This process consists in coupling, one after the other and in the order of the sequence of the GRF, 1) on the one hand, the following fragments : H-Ala-Arg-Ala-Arg-Leu-NH2 called Fragment A hGRF (40-44)or alaninamide (40) H-Gln-Glu-Arg-Gly-OH " " B'1 hGRF (36-39) H-Glu-Ser-Asn-OH " " B'2 hGRF (33-35) H-Ser-Arg-Gln-Gln-Gly-OH " " C hGRF (28-32) H-Leu-Gln-Asp-Ile-Met-OH " " D' hGRF (23-27) H-Arg-Lys-Leu-OH " " E'1 hGRF (20-22) to obtain the peptide K1 [(hGRF (20-44)] on the corresponding peptide having the sequence (20-40) and 2) on the other hand, the following fragments : H-Gln-Leu-Ser-Ala called Fragment F1 hGRF (16-l9) H-Tyr-Arg-Lys-Val-Leu-Gly OH " " G1 hGRF (10-15) H-Ile-Phe-Thr-Asn-Ser-OH " " H1 hGRF ( 5- 9) to obtain the peptide J [hGRF (5-19)] and thereafter to couple together the peptides J and K1 in order to form the peptide having the sequence hGRF (5-44) or hGRF (5-40) and finally to couple the resulting peptide with the peptide H-Tyr-Ala-Asp-Ala-OH, called fragment I hGRF (1-4).

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