固相片段缩合法制备胸腺素α

摘要以固相多肽合成(SPPS)为基础,应用固相片段合成方法制备胸腺素α1。系统考察了不同分段方法、缩合时间、反应溶剂、缩合剂及乙酰化的不同顺序对片段缩合反应的影响。通过试验确定了最佳合成工艺条件:采用三段(1~10、11~18和19~28)分别合成方式,以V(DMF)/V(DCM)等于3.0的混合溶液为反应溶剂,HATU为缩合剂,N末端氨基先乙酰化后进行片段间缩合的途径进行合成,多肽片段间缩合反应时间采用20.0 h。该条件下合成的胸腺素α1,粗品收率达64.3%,纯度达61.1%,与逐步合成法相比较,产物纯度提高了29.9%。

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	王炜
	张鸿鹏
	黄鹤

关键词：胸腺素α1 固相多肽合成固相片段缩合

Abstract： Based on solid-phase peptide synthesis,thymosin α_1(Tα_1) was synthesized by solid phase convergent synthesis.The effects of convergent protocol,coupling time,coupling solvents,coupling reagents and acetylation ways on the yield of Tα_1 were studied.The optimal protocol was obtained.Using the sequential condensation of three protected peptide segments(1—10,11—18,19—28),20.0 h as the coupling time,mixture of V(DMF)/V(DCM)=3.0 as the coupling solvent,HATU as the coupling reagent,the yield of crude thymosin α_1 was 64.3% with a purity of 61.1%.Compared with solid-phase peptide synthesis,the purity of thymosin α_1 synthesized by solid-phase convergent synthesis was increased by 29.9%.

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Received 2008-07-15; published 2008-07-15

引用本文:

王炜;张鸿鹏;黄鹤;.固相片段缩合法制备胸腺素α_1的工艺[J]. 化学工业与工程, 2008,25(4): 310-313

WANG Wei,ZHANG Hong-peng,HUANG He.Synthesis Technics of Thymosin α_1 by Solid Phase Convergent Peptide[J]. Chemcial Industry and Engineering, 2008,25(4): 310-313