环七肽PT-141的固相合成工艺研究  

Solid Phase Synthesis of Cyclo-heptapeptide PT-141

作　　者：宋芸[1] 李瑞敏[1] 宋扬[1] 

机构地区：[1]海南医学院海南省热带药用植物研发重点实验室,海南海口571199

出　　处：《广州化工》2016年第17期61-63,共3页GuangZhou Chemical Industry

基　　金：国家自然科学基金(20702036);高等学校博士学科点专项基金(20070056045)

摘　　要：PT-141可有望作为治疗性功能障碍的环七肽药物。本文研究了固相合成法合成PT-141的路线及工艺,氨基酸的α-氨基采用9-芴甲氧羰基(Fmoc)保护,以HBTU/HOBT/NMM为肽合成试剂,用高压制备液相色谱对粗品进行纯化,用质谱仪对合成的多肽进行结构鉴定。多肽合成的收率可达58%,纯化后可得纯度为98%的目标环七肽。与文献方法相比,该法简便、环境友好,并大幅降低了合成成本,适合产业化生产。Cyclo-heptapeptide PT-141 is expected to be a drug for the treatment of sexual dysfunction. The solidphase synthetic route to PT- 141 and the synthesizing process were studied. The α- amino acid was protected by Fmoc group,and the peptide was coupled by HBTU / HOBT / NMM in DMF. The obtained crude peptide was purified and then identified by the preparation HPLC and mass spectroscopy,respectively. With the synthetic route for the 58% yield,the purity of the obtained peptide could reach to 98%. The method is rapid and simple,low cost and environmental friendly,and it＇s fit for the large-scale production compared to the reported method.

关 键 词：环七肽 固相合成 9-芴甲氧羰基 固相环合 

分 类 号：TS197[轻工技术与工程—纺织化学与染整工程]