有机化学 ›› 2005, Vol. 25 ›› Issue (05): 604-607. 上一篇    下一篇

研究简报

Sansalvamide A固相合成新方法

刘守信*,1,2,冯霄1,耿艳楼2,姚军2,李军章2   

  1. (1西安交通大学环境与化学工程学院 西安 710049)
    (2河北科技大学化学与制药工程学院 石家庄 050018)
  • 收稿日期:2004-07-12 修回日期:2005-03-21 发布日期:2004-04-30
  • 通讯作者: 刘守信

Novel Solid-phase Synthetic Method of Sansalvamide A

LIU Shou-Xin*,1,2,FENG Xiao1,GENG Yan-Lou2,YAO Jun2,LI Jun-Zhang2   

  1. (1 College of Environment and Chemical Engineering, Xi'an Jiaotong University, Xi'an 710049)
    (2 College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018)
  • Received:2004-07-12 Revised:2005-03-21 Published:2004-04-30
  • Contact: LIU Shou-Xin

报道了Pd催化丁基二乙基硅烷树脂与N-Boc-4-溴代苯丙氨酸甲酯直接反应形成Si—Ar键一步构建出硅基连接分子的新方法, 并采用Boc策略增长肽链, 以PyBOP (benzotriazole-1-yl-oxy-tris-pyrrolidino-phosphonium hexafluoro- phosphate)为环合剂固相合成了sansalvamide A.

关键词: 固相合成, sansalvamide A, 硅基连接分子, 环肽类, Pd催化剂

It was reported that butyldiethylsilane polystyrene reacted with N-Boc-4-bromophenylalanine under palladium catalyzation to directly form silicon-linker with silicon aryl carbon bond. The peptide chain was elongated by using Boc strategy. And sansalvamide A was obtained by solid phase synthesis using PyBOP (benzotriazole-1-yl-oxy-tris-pyrrolidino-phosphonium hexafluoro- phosphate) as cyclization reagent.

Key words: silicon-linker, sansalvamide A, palladium catalyst, cyclic peptide, solid phase synthesis