Method for the manufacture of degarelix

Method for the manufacture of degarelix

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 s...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: ZHANG HAIXIANG, STAERKAER GUNNAR, FOMSGAARD JENS
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
container_end_page
container_issue
container_start_page
container_title
container_volume
creator ZHANG HAIXIANG
STAERKAER GUNNAR
FOMSGAARD JENS
description 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.
format Patent
fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_US8828938B2</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>US8828938B2</sourcerecordid><originalsourceid>FETCH-epo_espacenet_US8828938B23</originalsourceid><addsrcrecordid>eNrjZFD3TS3JyE9RSMsvUijJSFXITcwrTUtMLiktSlXIT1NISU1PLErNyazgYWBNS8wpTuWF0twMCm6uIc4euqkF-fGpxQWJyal5qSXxocEWFkYWlsYWTkbGRCgBAEWgJ6o</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Method for the manufacture of degarelix</title><source>esp@cenet</source><creator>ZHANG HAIXIANG ; STAERKAER GUNNAR ; FOMSGAARD JENS</creator><creatorcontrib>ZHANG HAIXIANG ; STAERKAER GUNNAR ; FOMSGAARD JENS</creatorcontrib><description>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.</description><language>eng</language><subject>CHEMISTRY ; METALLURGY ; ORGANIC CHEMISTRY ; PEPTIDES</subject><creationdate>2014</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20140909&amp;DB=EPODOC&amp;CC=US&amp;NR=8828938B2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76318</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20140909&amp;DB=EPODOC&amp;CC=US&amp;NR=8828938B2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>ZHANG HAIXIANG</creatorcontrib><creatorcontrib>STAERKAER GUNNAR</creatorcontrib><creatorcontrib>FOMSGAARD JENS</creatorcontrib><title>Method for the manufacture of degarelix</title><description>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.</description><subject>CHEMISTRY</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PEPTIDES</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2014</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZFD3TS3JyE9RSMsvUijJSFXITcwrTUtMLiktSlXIT1NISU1PLErNyazgYWBNS8wpTuWF0twMCm6uIc4euqkF-fGpxQWJyal5qSXxocEWFkYWlsYWTkbGRCgBAEWgJ6o</recordid><startdate>20140909</startdate><enddate>20140909</enddate><creator>ZHANG HAIXIANG</creator><creator>STAERKAER GUNNAR</creator><creator>FOMSGAARD JENS</creator><scope>EVB</scope></search><sort><creationdate>20140909</creationdate><title>Method for the manufacture of degarelix</title><author>ZHANG HAIXIANG ; STAERKAER GUNNAR ; FOMSGAARD JENS</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US8828938B23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2014</creationdate><topic>CHEMISTRY</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PEPTIDES</topic><toplevel>online_resources</toplevel><creatorcontrib>ZHANG HAIXIANG</creatorcontrib><creatorcontrib>STAERKAER GUNNAR</creatorcontrib><creatorcontrib>FOMSGAARD JENS</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>ZHANG HAIXIANG</au><au>STAERKAER GUNNAR</au><au>FOMSGAARD JENS</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Method for the manufacture of degarelix</title><date>2014-09-09</date><risdate>2014</risdate><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.</abstract><oa>free_for_read</oa></addata></record>
fulltext fulltext_linktorsrc
identifier
ispartof
issn
language eng
recordid cdi_epo_espacenet_US8828938B2
source esp@cenet
subjects CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
title Method for the manufacture of degarelix
url https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-11T17%3A58%3A44IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-epo_EVB&rft_val_fmt=info:ofi/fmt:kev:mtx:patent&rft.genre=patent&rft.au=ZHANG%20HAIXIANG&rft.date=2014-09-09&rft_id=info:doi/&rft_dat=%3Cepo_EVB%3EUS8828938B2%3C/epo_EVB%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true