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发明公开
CN104478886A 一种富勒烯双加成氨基酸及其合成方法 无效 - 驳回

一种富勒烯双加成氨基酸及其合成方法
摘要：
本发明公开了一种富勒烯双加成氨基酸及其合成方法，将富勒烯双加成吡咯烷与带有保护基的氨基酸溶于DCM/DMF混合液中，然后加入HOBT、DCC和DMAP，在常温下反应20~100小时，柱层析分离后得到带有保护基的富勒烯双加成氨基酸；将得到的带有保护基的富勒烯双加成氨基酸加入TFA/DCM混合液中进行保护基的脱除，反应1~10小时，加入冰乙醚，得沉淀离心干燥后得到富勒烯双加成氨基酸。本发明的富勒烯双加成氨基酸具有良好的水溶性和生物相容性，大大提高了富勒烯在极性溶液中的溶解度，并具有良好的抗癌活性；优良的去除自由基方面性能；本发明的合成方法可适用于很多种氨基酸，进而得到多种富勒烯双加成氨基酸衍生物。
摘要（英）：

The invention discloses a fullerene biaddition amino acid and a synthetic method thereof. The synthetic method comprises the following steps: dissolving fullerene biaddition pyrrolidine and amino acid with a protecting group in a DCM/DMF mixed liquid, adding HOBT, DCC and DMAP to react for 20-100 hours at room temperature, and performing column chromatography isolation to obtain fullerene biaddition amino acid with the protecting group; adding the obtained fullerene biaddition amino acid with the protecting group in a TFA/DCM mixed liquid to remove the protecting group, reacting for 1-10 hours, and adding frozen diethyl ether to obtain settled, centrifugal and dried fullerene biaddition amino acid. The fullerene biaddition amino acid has excellent water solubility and biocompatibility, so that the solubility of fullerene in a polar solution is greatly improved, and the antitumor activity is excellent; the performance of removing the protecting group is excellent; the synthetic method can be suitable for various amino acids, so that various fullerene biaddition amino acid derivatives are obtained.

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