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
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung: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.