申请人:Chugai Seiyaku Kabushiki Kaisha
公开号:EP3636656A1
公开(公告)日:2020-04-15
Methods of producing a peptide containing an N-substituted amino acid or N-substituted amino acid analog of the present invention include the steps of:
preparing an Fmoc-protected amino acid, an Fmoc-protected amino acid analog, or an Fmoc-protected peptide;
deprotecting a protecting group which have an Fmoc skeleton of the Fmoc-protected amino acid and such by using a base; and
forming an amide bond by adding a new Fmoc-protected amino acid and such;
and when the peptide is produced by a solid-phase method, the obtained peptide is cleaved off from the solid phase under conditions of weaker acidity than TFA. Furthermore, at least one side chain of the obtained peptide has a protecting group that is not deprotected under basic conditions and is deprotected under conditions of weaker acidity than TFA.
生产含有本发明的N-取代氨基酸或N-取代氨基酸类似物的多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;
使用碱对具有 Fmoc 骨架的 Fmoc 保护氨基酸的保护基进行脱保护;以及
通过添加新的 Fmoc 保护氨基酸形成酰胺键;
当采用固相法生产多肽时,在酸性比反式脂肪酸弱的条件下从固相中裂解得到多肽。此外,所得多肽的至少一个侧链具有保护基团,该保护基团在碱性条件下未被脱保护,而在酸性弱于 TFA 的条件下被脱保护。