METHOD FOR SYNTHESIZING DOPA OLIGOPEPTIDE INTERMEDIATE AND USE, COMPOSITION AND PREPARATION THEREOF
This invention belongs to the medicine field and discloses a synthetic method of L-DOPA-containing oligopeptide derivatives and pharmaceutical applications. Specifically, it includes an improved synthesis of ketal-protected L-DOPA intermediates, the synthesis of fatty acid conjugates with L-DOPA-con...
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creator | HE, Yanmiao ZHONG, Shibo LIU, Zhongqiang CHEN, Sikang HU, Bihuang ZHANG, Xiaoyan NING, Donghua WAN, Ying LI, Mengdi FAN, Lixia XIONG, Feng FU, Kaizhong YAO, Rui |
description | This invention belongs to the medicine field and discloses a synthetic method of L-DOPA-containing oligopeptide derivatives and pharmaceutical applications. Specifically, it includes an improved synthesis of ketal-protected L-DOPA intermediates, the synthesis of fatty acid conjugates with L-DOPA-containing dipeptides using the above key intermediates. The said ketal-protected intermediate can be synthesized in two steps with high yields, eliminating the two steps of protection and deprotection of a carboxyl group used in the previous art. This intermediate was applied to synthesize many end products, and among them, FDD-16, FDD-18 and FDD-14 can form gels in a wide range of concentrations, which exhibit good stabilities and long half-lives and are promising to be developed into anti-parkinsonism drugs with high bioavailability and long-term controlled-release effect. |
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Specifically, it includes an improved synthesis of ketal-protected L-DOPA intermediates, the synthesis of fatty acid conjugates with L-DOPA-containing dipeptides using the above key intermediates. The said ketal-protected intermediate can be synthesized in two steps with high yields, eliminating the two steps of protection and deprotection of a carboxyl group used in the previous art. This intermediate was applied to synthesize many end products, and among them, FDD-16, FDD-18 and FDD-14 can form gels in a wide range of concentrations, which exhibit good stabilities and long half-lives and are promising to be developed into anti-parkinsonism drugs with high bioavailability and long-term controlled-release effect.</description><language>eng ; fre ; ger</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PEPTIDES ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2022</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&date=20221207&DB=EPODOC&CC=EP&NR=3929183A4$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76289</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20221207&DB=EPODOC&CC=EP&NR=3929183A4$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>HE, Yanmiao</creatorcontrib><creatorcontrib>ZHONG, Shibo</creatorcontrib><creatorcontrib>LIU, Zhongqiang</creatorcontrib><creatorcontrib>CHEN, Sikang</creatorcontrib><creatorcontrib>HU, Bihuang</creatorcontrib><creatorcontrib>ZHANG, Xiaoyan</creatorcontrib><creatorcontrib>NING, Donghua</creatorcontrib><creatorcontrib>WAN, Ying</creatorcontrib><creatorcontrib>LI, Mengdi</creatorcontrib><creatorcontrib>FAN, Lixia</creatorcontrib><creatorcontrib>XIONG, Feng</creatorcontrib><creatorcontrib>FU, Kaizhong</creatorcontrib><creatorcontrib>YAO, Rui</creatorcontrib><title>METHOD FOR SYNTHESIZING DOPA OLIGOPEPTIDE INTERMEDIATE AND USE, COMPOSITION AND PREPARATION THEREOF</title><description>This invention belongs to the medicine field and discloses a synthetic method of L-DOPA-containing oligopeptide derivatives and pharmaceutical applications. 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Specifically, it includes an improved synthesis of ketal-protected L-DOPA intermediates, the synthesis of fatty acid conjugates with L-DOPA-containing dipeptides using the above key intermediates. The said ketal-protected intermediate can be synthesized in two steps with high yields, eliminating the two steps of protection and deprotection of a carboxyl group used in the previous art. This intermediate was applied to synthesize many end products, and among them, FDD-16, FDD-18 and FDD-14 can form gels in a wide range of concentrations, which exhibit good stabilities and long half-lives and are promising to be developed into anti-parkinsonism drugs with high bioavailability and long-term controlled-release effect.</abstract><oa>free_for_read</oa></addata></record> |
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subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
title | METHOD FOR SYNTHESIZING DOPA OLIGOPEPTIDE INTERMEDIATE AND USE, COMPOSITION AND PREPARATION THEREOF |
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