Synthesis method of intermediate of dopa oligopeptide, application of intermediate, composition and preparation

The invention belongs to the field of medicines, and discloses a synthesis method of an intermediate of dopa oligopeptide, application of the intermediate, a composition and a preparation. The invention particularly relates to improvement of a synthesis method of a ketal-protected L-DOPA intermediat...

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Hauptverfasser: HE YANMIAO, YAO RUI, CHEN SIKANG, FU KAIZHONG, ZHANG XIAOYAN, LI MENGDI, ZHONG SHIBO, NING DONGHUA, LIU ZHONGQIANG, FAN LIXIA, XIONG FENG, HU BIHUANG, WAN YING
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the field of medicines, and discloses a synthesis method of an intermediate of dopa oligopeptide, application of the intermediate, a composition and a preparation. The invention particularly relates to improvement of a synthesis method of a ketal-protected L-DOPA intermediate and synthesis of oligopeptides and fatty acid derivatives containing L-DOPA by using the key intermediate. The medical intermediate can be prepared by only two steps, two-step reaction of carboxyl protection and deprotection is avoided, and the yield is high; the final products synthesized by using the intermediate, especially FDD-16, FDD-18 and FDD-14, have wide gel forming concentration range, have good stability and long half-life period, are expected to be developed into a long-acting Parkinson's disease treatment drug with high bioavailability, and are suitable for further drug development and use. 本发明属于药物领域,公开了一种多巴寡肽的中间体的合成方法及其用途、组合物和制剂。具体涉及缩酮保护的L-DOPA中间体的合成方法改进,以及使用该关键中间体合成含L-DOPA的寡肽和脂肪酸衍生物。所述的医药中间体仅需要二步就能