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有机化学
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有机化学 ›› 2000, Vol. 20 ›› Issue (3): 419-423. 上一篇    下一篇

研究论文

Boc和Fmoc保护氨基酸与M树脂和王氏树脂结合率的比较

张志刚;白玲;蔡豪斌;何水淋   

  1. 桂林医学院生化教研室;桂林医学院生物工程研究所
  • 发布日期:2000-06-25

A comparison between the yield of the attachment of Boc-AA-O^-Cs^+ to merrifield resin and of Fmoc-AA-OH to Wang resin

Zhang Zhigang;Bai Ling;Cai Haobin;He Shuilin   

  • Published:2000-06-25

PDF

630

被引次数

34

M树脂与Boc保护的亮氨酸、甘氨酸或苯丙氨酸的铯盐成酯反应摩尔比1:1.2,时间31h,其产物用重量法和水杨醛法测得的结合率均值分别为87.3%、89.1%和89.6%。王氏树脂与Fmoc保护的亮氨酸、甘氨酸或苯丙氨酸反应48h,树脂:Fmoc氨基酸:DCC:DMAP摩尔比为1:3:4:1,其产物结合率的均值分别为44.2%、30.4%和56.2%。结果表明,前者产物结合率高于后者。另外,重量法与水杨醛法测得的结合率相差不超过2.7%,但重量法更方便,易行。

关键词: 叔丁氧羰基, 芴甲氧羰基, 端基保护, 氨基酸, 多肽4, 固相合成, 树脂, 结合, 铯化合物

The yields of the attachment of Boc-Lue-O^-Cs^+, Boc-Gly-O^-Cs^+ or Boc-Phe-O^-Cs^+(1.2 eqv.) to Merrifield resin (1.0eqv.) for 31 hours is 87.3%, 89.1% or 89.6% (the mean values of those detected by weight and by these measured the free amino group, respectively). The yields of the anchoring of Fmoc-Lue-OH, Fmoc-Gly-OH or Fmoc-Phe-OH (3.0 eqv. ) to Wang resin (1.0 eqv.) for 48 hours is 44.2%, 30.4% or 56.2% (the mean values of those detected by weight and those measured by the free amino group, respectively). The results show that the combination ratio of Boc-strategy is at least 33.4% higher than that of the Fmoc-strategy. In addition, difference in the combination ratios between those determined by weight and the those by the free amino group is below 2.7%, but weight method is more convenient and feasible.

Key words: AMINO ACID, SOLIDPHASE SYNTHESIS, RESIN, BINDING, CESIUM COMPOUNDS

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