建立了抗肿瘤肽AP-9的Fmoc固相全合成方法,产品纯度大于98%。着重研究了Fmoc-Arg(Pbf)-OH与H—Pro—Trt树脂的缩合反应。结果表明,以THF-NMP(1:1)为溶剂,于30℃微波辐射反应6min,缩合产率达80.2%。
Antitumor peptide AP-9 (YKLPGHHHHYRP) was synthesized by Fmoc-solid phase peptide synthesis, and the purity of the product was more than 98 %. The coupling reaction between the difficult sequence Fmoc- Arg (Pbf)-OH and H-Pro-Trt resin was investigated. The results showed that the coupling reaction could be completed when it was carried out for 6min at 30℃ by microwave irradiation with THF-NMP (1 : 1) as the solvent, and the yield could reach to 80.2 %.