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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Hauptverfasser: 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
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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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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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