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Synthesis of polypeptide by a thioester method

机译：通过硫酯法合成多肽法

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We have been developing a method of protein synthesis using peptide thioesters as building blocks and have reported syntheses of proteins by the method [1-5]. The synthetic procedure, however, becomes complicated, if a protein contains cysteine residues, since it becomes necessary to prepare a segment having benzyl-type protecting groups using an Npys solid-phase method and which are stable to silver ions [5]. The acetamidomethyl (Acm) group represents a more ideal blocking group for the mercapto group of a cysteine residue, since it is more easily prepared usign a solid-phase method by Boc-strategy. If we could find the reaction conditions which allow a coupling reaction to proceed at a reasonable rate and under which the Acm group is stable toward silver ions, a simple and general method could be developed for the synthesis of cysteine-containing proteins.
机译：我们一直在开发一种蛋白质合成方法，使用肽硫酯作为结构块，并通过该方法报道了蛋白质的合成[1-5]。然而，如果蛋白质含有半胱氨酸残基，则合成程序变得复杂化，因为必须使用NPYS固相法制备具有苄基型保护基团的区段并且稳定于银离子[5]。乙酰氨基甲酰基（ACM）基团代表半胱氨酸残基的巯基的更理想的封闭基团，因为它通过Boc策略更容易制备了使用固相方法。如果我们能够发现允许偶联反应的反应条件以合理的速率进行，并且在其下，ACM基团对银离子稳定，可以开发简单且一般的方法以合成含半胱氨酸的蛋白质。

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