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題 名 | Convenient Solid-phase Synthesis of Tyr[fec4]-octreotide |
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作 者 | Lee,Te-wei; Chang,Shiang-rong; Chen,Shui-tein; Tsai,Zei-tsan; | 書刊名 | 中央研究院生物化學研究所論文集 |
卷 期 | 24 1998[民87.] |
頁 次 | 頁35-40 |
分類號 | 361.4 |
關鍵詞 | Solid-phase synthesis; Tyr[fec4]-octreotide; |
語 文 | 英文(English) |
英文摘要 | We have developed a new method to anchor Thr(ol) to a solid-phase synthesis resin for preparation of Tyr �� -octreotide. Fmoc-Thr(ol)-terephthal-acetal, prepared from Fmoc-Thr-OH. was loaded onto the resin. After construction of the peptide chains by Fmoc chemistry, cyclization of the peptide may be obtained on-resin by oxidation with iodine in DMF. The cleavage of the peptide-resin with trifluoroacetic acid, followed by the reverse-phase HPLC purification, produced Tyr �� -octreotide with an overall yield of 40% from the starting Fmoc-Thr(ol)-terephthal-acetal-resin. The final product gave a single peak on analytical HPLC and electrospray mass spectrometry confirmed the integrity of the product. Iodine-123 radiolabeling of the product provided �騁滋� l-Tyr �� -octreotide with >98@/@ radiochemical purity. |
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