胸腺素α1的Fmoc固相合成法

Fmoc Solid-phase Synthesis of Thymosin α1

本文用Fmoc固相方法合成了胸腺素α1。采用对碱敏感的Fmoc作为α -氨基的保护基 ,并确定与之配套的侧链保护策略。探索出了适宜的接肽方案 ,即前 9步接肽用对称酸酐法 ,后 1 8步用DCC -HOBt缩合法 ,从而保证了每步的高缩合率。试验结果表明各步的缩合率均在 96 2 %以上 ,多数达 99%以上。同时还对合成工艺条件进行了研究。合成粗品的纯度 (胸腺素α1的含量 )为 46 52 % (质量分数 ) ,胸腺素收率为 37 81 %

In this thesis, the thymosin α1 has been synthesized by a solid-phase method. Using the base-labile Fmoc group to protect the α-amino acid, and present a strategy for the synthesis of a thymosin α1. Then a suitable synthesis method is determinedie, that is using preformed symmetrical anhydrides(PSA)in the first 9 synthesis steps, using DCC-HOBt chemistry coupling in the next 18 steps. The result shows that the yield of the coupling synthesis of each step is over 96.2%, most of them are over 99%. Meanwhile, technology conditions of synthesis were studied. The purification of our product (the content of Tα1) is 46.52%, the yield of it is 37.81%.