| 摘要 |
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): (P)AA-AA-AA(III) or a salt thereof with a second polypeptide of formula (IV): AA(P)-AA-AA(P)-AA-AA(P)-AA-AA-NH(IV), or its salt in a liquid reaction medium in presence of a peptide coupling agent to obtain a decapeptide of formula (II): (P)AA-AA-AA-AA(P)-AA-AA(P)-AA-AA(P)-AA-AA-NH(II), where P, Peach independently denotes hydrogen or a protective group; P, P, each independently represents a protective group; AArepresents a D-2Nal; AArepresents a D-4Cpa; AArepresents a D-3Pal; AAis Ser; AArepresents 4Aph (L-Hor); AArepresents a D-Aph (Cbm); AArepresents Leu; AArepresents a Lys (iPr); AArepresents Pro; AArepresents D-Ala.EFFECT: disclosed method enables large-scale production of degarelix.12 cl, 12 dwg, 6 tbl, 5 ex |
