Two steps are postulated in a new method of intramolecular peptide synthesis using oxalic acid derivatives (Fig. 1). Both are verified with model derivatives incorporating one sarcosine residue: cyclisation of 2d into 5 (Fig. 4) and aminolysis of 5 leading to 2h (Fig. 5). Glycine, alanine and phenyl- alanine derivatives however are not cyclizised in the studied conditions (attempted acid-, by trifluoroacetic
在使用
草酸衍
生物的分子内肽合成的新方法中假定了两个步骤(图1)。两者均通过包含一个
肌氨酸残基的模型衍
生物进行了验证:将2d环化为5(图4),将5进行
氨解导致2h(图5)。但是,在所研究的条件下(甘
氨酸,丙
氨酸和苯基丙
氨酸衍
生物)(
三氟乙酸尝试过酸,
三乙胺进行碱性催化)没有被环化,这排除了该方法的一般用途。