New peptide fragment is prepared by loading fluorenylmethoxycarbonyl protecting group protected threonine to resin solid-phase support, protecting with suitable protecting group, in the presence of coupling agent, and de-protecting using de-protecting agent for preparation of Semaglutide
	KODIDASU A; VABILISETTI N; GALIPALLI R; PONNUSAMY T; RAMU V G; MANDAPATI B
	2023-09-07
专利权人	ALEMBIC PHARM LTD (ALEM-C)
申请日期	2023-09-07
专利号	IN202321060136-A
成果简介	NOVELTY - Peptide fragment is new, where peptide fragment comprises 4 amino acid sequence (SEQ ID NO: 1), given in the specification, or a pharmaceutically acceptable salt. USE - Peptide fragment for preparation of Semaglutide. DETAILED DESCRIPTION - Peptide fragment is new, where peptide fragment comprises 4 amino acid sequence 2-Aminoisobutyric acid (Aib)-Glu-Gly-Thr-OH (SEQ ID NO: 1), or a pharmaceutically acceptable salt. INDEPENDENT CLAIMS are included for: Method for preparation of Semaglutide or a pharmaceutically acceptable salt, which involves: (a) loading of Fmoc protected glycine to a resin solid-phase support in the presence of coupling agent and a catalyst; (b) de-protection of fluorenylmethoxycarbonyl protecting group (Fmoc) using de-protecting agent and sequential coupling of amino acids with N-terminal protection and side chain protection based on the sequence of peptide backbone of Semaglutide till Phe12 in the presence of coupling agent to obtain Fmoc-Phe12-Thr13-Ser14-Asp15-Val16-Ser17-Ser18-Tyr19-Leu20-Glu21-Gly22-Gln23-Ala24-Ala25-Lys26[Xn]-Glu27-Phe28-Ile29-Ala30-Trp31-Leu32-Val33-Arg34-Gly35-Arg36-Gly37-Resin, where Xn is selected from Alloc, Mtt, Dde, Mmt and ivDde; (c) de-protecting Fmoc protecting group of fragment obtained in step (b) using de-protecting agent followed by coupling of tetra-peptide fragment Aib8-Glu9-Gly10-Thr11-OH (SEQ ID-1) where, the side chain of amino acids protected with a suitable protecting group, in the presence of coupling agent, to obtain Fmoc-Aib8-Glu9-Gly10-Thr11-Phe12-Thr13-Ser14-Asp15-Val16-Ser17-Ser18-Tyr19-Leu20-Glu21-Gly22-Gln23-Ala24-Ala25-Lys26[Xn]-Glu27-Phe28-Ile29-Ala30-Trp31-Leu32-Val33-Arg34-Gly35-Arg36-Gly37-Resin; (d) de-protecting Fmoc protecting group using de-protecting agent and coupling of N-terminal and side chain protected histidine, in the presence of coupling agent, to obtain His7-Aib8-Glu9-Gly10-Thr11-Phe12-Thr13-Ser14-Asp15-Val16-Ser17-Ser18-Tyr19-Leu20-Glu21-Gly22-Gln23-Ala24-Ala25-Lys26[Xn]-Glu27-Phe28- Ile29-Ala30-Trp31-Leu32-Val33-Arg34-Gly35-Arg36-Gly37-Resin; and (e) de-protecting protecting group (Xn) from Lys26, to obtain His7-Aib8-Glu9-Gly10-Thr11-Phe12-Thr13-Ser14-Asp15-Val16-Ser17-Ser18-Tyr19-Leu20-Glu21-Gly22-Gln23-Ala24-Ala25-Lys26-Glu27-Phe28-Ile29-Ala30-Trp31-Leu32-Val33-Arg34-Gly35- Arg36-Gly37-Resin and converting the resulting peptide to semaglutide; and Method for preparation of peptide fragment having amino acids sequence SEQ ID NO: 1 or pharmaceutically acceptable salt.
IPC 分类号	A61K-009/00 ; B32B-003/26 ; C07C-045/68 ; C07F-009/12 ; C07K-014/605
国家	印度
专业领域	医药卫生
语种	英语
成果类型	专利
文献类型	科技成果
条目标识符	http://119.78.100.226:8889/handle/3KE4DYBR/20471
专题	中国科学院新疆生态与地理研究所
作者单位	ALEMBIC PHARM LTD (ALEM-C)
推荐引用方式 GB/T 7714	KODIDASU A,VABILISETTI N,GALIPALLI R,et al. New peptide fragment is prepared by loading fluorenylmethoxycarbonyl protecting group protected threonine to resin solid-phase support, protecting with suitable protecting group, in the presence of coupling agent, and de-protecting using de-protecting agent for preparation of Semaglutide. IN202321060136-A[P]. 2023.

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