Invention Grant
- Patent Title: Method for the manufacture of degarelix
- Patent Title (中): 地加瑞克的制造方法
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Application No.: US13265402Application Date: 2010-04-26
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Publication No.: US08828938B2Publication Date: 2014-09-09
- Inventor: Haixiang Zhang , Jens Fomsgaard , Gunnar Staerkaer
- Applicant: Haixiang Zhang , Jens Fomsgaard , Gunnar Staerkaer
- Applicant Address: DK Hillerod
- Assignee: Polypeptide Laboratories A/S
- Current Assignee: Polypeptide Laboratories A/S
- Current Assignee Address: DK Hillerod
- Agency: Dickstein Shapiro LLP
- Priority: SE0900558 20090424
- International Application: PCT/EP2010/002550 WO 20100426
- International Announcement: WO2010/121835 WO 20101028
- Main IPC: C07K7/23
- IPC: C07K7/23

Abstract:
In a step-wise synthesis of degarelix comprising 0.3% by weight or less of 4-([2-(5-hydantoyl)]acetylamino)-phenylalanine analog on (solid support)-NH2 a step comprises providing a solution of an amino acid or peptide of which the α-amino group is protected by Fmoc; contacting the support with the solution in the presence of reagent for forming a peptide bond between a carboxyl group of the amino acid or peptide and (solid support)-NH2; removing Fmoc by contacting the support with an organic base, in particular piperidine, in an organic solvent. Also disclosed is degarelix of high purity prepared by the method of the invention and the use of Fmoc in the synthesis of degarelix.
Public/Granted literature
- US20120041172A1 METHOD FOR THE MANUFACTURE OF DEGARELIX Public/Granted day:2012-02-16
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