反应时间、温度和溶剂对缬氨酸自组装成聚合肽反应的影响

寡肽类化合物一般具有较强的生物活性，多数可作为药物或药物前体，因此成为人们的研究热点之一．目前寡肽的合成方法主要有液相法、固相法及酶促合成法，这些合成方法往往需要对氨基酸的活性基团进行选择性保护，步骤繁琐．近期研究发现，在水-醇体系中α-氨基酸被磷酰化为N-磷酰-α-氨基酸后，可发生自组装聚合肽反应；在无水条件下，N，O-二(三甲基硅基)-α-氨基酸可与磷酰化试剂如O，O-亚苯基磷酰氯反应生成N-磷酰-α-氨基酸，后者也可通过自组装反应得到二～八肽，但这些N-磷酰-α-氨基酸的制备均需使用有机磷试剂．我们发现，在无机磷试剂如PCl5等辅助下，α-氨基酸同样可以发生自组装反应，得到一系列寡聚肽，这既可为寡聚肽的合成提供一种新的方法，同时，因无机磷试剂在原始地球条件下更可能存在，因而对于揭示多肽及蛋白质的起源具有重要意义．氨基酸的自组装反应具有链锁反应的特点，因此必须控制反应条件实现对反应的控制。

Influence of Reaction Time, Temperature and Solvent on the Self-assembly into Oligo-peptides for Valine

Owing to having very strong bioactivity, oligo-peptides can be used as the medication or the pre-medication and become the studying focus now. Existing methods for synthesizing oligo-peptides included liquid phase peptide synthesis, solid phase peptide synthesis and enzymatic peptide synthesis. In this paper, a new method for synthesizing oligo-peptides by phosphorus oxychloride activation was reported. With the assistance of phosphorus oxychloride, the phosphorylation of L-valine could take place and then was assembled into oligo-peptides, which were analyzed by electrospray ionization mass spectrometry(ESI-MS). On quenching with methanol, the reaction mixtures, which were produced under different reaction conditions, yielded the corresponding peptide methyl esters. Moreover, we found that, as the reaction conditions such as reaction time, solvent and temperature were changed, the length of peptides changed. And the length of peptides could be controlled by changing the reaction conditions.