炔基修饰的紫杉醇衍生物的合成
首发时间:2024-04-09
摘要:紫杉醇是临床常见抗肿瘤药物,但紫杉醇水溶性较差需要进行修饰改造。本实验旨在通过酯化反应将紫杉醇和4-戊炔酸相偶联,合成一种新的紫杉醇衍生物。通过液相色谱-质谱联用技术(LC-MS)对产物进行了表征。通过水溶性测定实验,测定了该衍生物在水中的溶解度。该实验在紫杉醇上引入炔基进行修饰,合成了一种新的中间产物,该产物可以进一步与多肽、聚乙二醇等偶联,增强紫杉醇的水溶性,便于进一步改善紫杉醇剂型,提高生物利用度。
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Synthesis of acetylene modified paclitaxel derivatives
Abstract:Paclitaxel is a common anti-tumor drug in clinical practice, but it has many drawbacks that require modification and modification. The aim of this experiment is to couple paclitaxel and 4Coupling synthesis of paclitaxel and 4-pentyne acid-pentyne acid through esterification reaction to synthesize a new compound. Through this experiment, we hope to explore the synthesis method of the new compound and preliminarily evaluate its structure and potential biological activity. The synthesized product was characterized by liquid chromatography-mass spectrometry (LC-MS). The experimental results showed that the esterification coupling product of paclitaxel and 4-pentyne acid was successfully synthesized. The molecular weight matches the expected product, confirming the success of the synthesized compound. The successful synthesis of this compound provides a basis for further research on its biological activity and pharmacological properties. In addition, this experiment also demonstrated the importance of esterification reactions in organic synthesis and provided a method for further exploring the chemical modification and structural modification of paclitaxel.
Keywords: Medicinal chemistry Paclitaxel 4-Pentyne acid Esterification reaction
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