- Patent Title: Method for synthesizing peptide containing N-substituted amino acid
-
Application No.: US16619388Application Date: 2018-06-08
-
Publication No.: US11542299B2Publication Date: 2023-01-03
- Inventor: Kenichi Nomura , Terushige Muraoka , Mikimasa Tanada , Takashi Emura
- Applicant: Chugai Seiyaku Kabushiki Kaisha
- Applicant Address: JP Tokyo
- Assignee: Chugai Seiyaku Kabushiki Kaisha
- Current Assignee: Chugai Seiyaku Kabushiki Kaisha
- Current Assignee Address: JP Tokyo
- Agency: Nixon & Vanderhye P.C.
- Priority: JPJP2017-114073 20170609
- International Application: PCT/JP2018/021998 WO 20180608
- International Announcement: WO2018/225851 WO 20181213
- Main IPC: C07K11/02
- IPC: C07K11/02 ; C07K1/06

Abstract:
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.
Public/Granted literature
- US20200277327A1 METHOD FOR SYNTHESIZING PEPTIDE CONTAINING N-SUBSTITUTED AMINO ACID Public/Granted day:2020-09-03
Information query