METHOD FOR PRODUCTION OF DEGARELIX AND INTERMEDIATE COMPOUNDS THEREOF Russian patent published in 2016 - IPC C07K1/02 C07K5/08 C07K7/06 C07K7/23 

FIELD: chemistry.

SUBSTANCE: invention relates to liquid-phase method of producing decapeptide - degarelix and intermediate compounds for producing decapeptide. Invention also relates to intermediate polypeptides for liquid-phase method of producing degarelix. Method is realised by combining a first polypeptide of formula (III): (P₁)AA₁-AA₂-AA₃ (III) or a salt thereof with a second polypeptide of formula (IV): AA₄(P₄)-AA₅-AA₆(P₆)-AA₇-AA₈(P₈)-AA₉-AA₁₀-NH₂ (IV), or its salt in a liquid reaction medium in presence of a peptide coupling agent to obtain a decapeptide of formula (II): (P₁)AA₁-AA₂-AA₃-AA₄(P₄)-AA₅-AA₆(P₆)-AA₇-AA₈(P₈)-AA₉-AA₁₀-NH₂ (II), where P₁, P₈ each independently denotes hydrogen or a protective group; P₄, P₆, each independently represents a protective group; AA₁ represents a D-2Nal; AA₂ represents a D-4Cpa; AA₃ represents a D-3Pal; AA₄ is Ser; AA₅ represents 4Aph (L-Hor); AA₆ represents a D-Aph (Cbm); AA₇ represents Leu; AA₈ represents a Lys (iPr); AA₉ represents Pro; AA₁₀ represents D-Ala.

EFFECT: disclosed method enables large-scale production of degarelix.

12 cl, 12 dwg, 6 tbl, 5 ex