哑铃型树枝状多肽大分子的合成

Synthesis of barbell-like peptide dendrimer

目的 合成哑铃型树枝状多肽大分子。方法 通过引入小分子化合物Fmoc-Gly-OH作为连接臂,高产率得到双端氨基化聚乙二醇（NH_2-CH_2-COO-PEG_（2000）-OOC-CH_2-NH_2）;然后再分别以双芴甲氧羰基保护的赖氨酸〔Fmoc-Lys（Fmoc）-OH〕、芴甲氧羰基及叔丁氧羰基保护的赖氨酸〔Fmoc-Lys（Boc）-OH〕为支化单元,采用液相发散法合成了表面富含氨基的哑铃型PEG/赖氨酸树枝状大分子共聚物。结果和结论 利用~1H NMR和MS对中间产物及终产物的结构和相对分子质量进行表征,结果表明成功合成了哑铃型树状多肽大分子,为其在生物医学领域的应用打下基础。

Objective To synthesize barbell-like peptide dendrimer. Methods Through the introduction of small molecule Fmoc-Gly-OH as the linker,NH_2-CH_2-COO-PEG_（2000）-OOC-CH_2-NH_2 was obtained efficiently. And then N-α-N-ε-di-Fmoc-L-lysine and N-α-Fmoc-N-ε-Boc-L-lysine were used as branching agents,and barbell-like poly（ethylene glycol）-block-poly（L-lysine）dendrimer with a large number of surface amino groups was synthesized by the liquid-phase peptide synthesis method and divergent approach. Results and Conclusion The structure and relative molecular mass of the final products and intermediates were characterized and confirmed by ~1H NMR and MS. The results revealed that barbell-like peptide dendrimer can be obtained by this method,which lays the foundation of its application in biological areas.