用于合成含有n-取代氨基酸的肽的方法

文档序号:1539140 发布日期:2020-02-14 浏览:20次 >En<

阅读说明:本技术 用于合成含有n-取代氨基酸的肽的方法 (Method for synthesizing peptides containing N-substituted amino acids ) 是由 野村研一 村冈照茂 棚田干将 江村岳 于 2018-06-08 设计创作,主要内容包括:生产本发明的含有N-取代的氨基酸或N-取代的氨基酸类似物的肽的方法,包括以下步骤:制备Fmoc保护的氨基酸、Fmoc保护的氨基酸类似物或Fmoc保护的肽;通过使用碱,使具有Fmoc保护的氨基酸等的Fmoc骨架的保护基脱保护;和通过添加新的Fmoc保护的氨基酸等,形成酰胺键;以及当通过固相方法生产肽时,在比TFA弱的酸度条件下将获得的肽从固相上切下。此外,所获得的肽的至少一个侧链具有保护基,该保护基在碱性条件下不被脱保护,并且在比TFA弱的酸性条件下被脱保护。(A method for producing a peptide of the present invention comprising an N-substituted amino acid or an N-substituted amino acid analog, comprising the steps of: preparing Fmoc-protected amino acids, Fmoc-protected amino acid analogs, or Fmoc-protected peptides; deprotecting a protecting group of Fmoc skeleton of an Fmoc-protected amino acid or the like by using a base; and forming an amide bond by adding a new Fmoc-protected amino acid or the like; and when the peptide is produced by a solid phase method, cleaving the obtained peptide from the solid phase under a condition of weaker acidity than TFA. Further, at least one side chain of the obtained peptide has a protecting group which is not deprotected under basic conditions and deprotected under acidic conditions weaker than TFA.)

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