CN114585636A - 一种普卡那肽的制备方法 - Google Patents

一种普卡那肽的制备方法 Download PDF

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Publication number
CN114585636A
CN114585636A CN202080003011.9A CN202080003011A CN114585636A CN 114585636 A CN114585636 A CN 114585636A CN 202080003011 A CN202080003011 A CN 202080003011A CN 114585636 A CN114585636 A CN 114585636A
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China
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fmoc
resin
leu
procainatide
cys
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CN202080003011.9A
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CN114585636B (zh
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马洪季
吴丽芬
张利香
付玉清
邱心敏
林艳霞
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SHENZHEN JYMED TECHNOLOGY CO LTD
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SHENZHEN JYMED TECHNOLOGY CO LTD
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

一种普卡那肽的制备方法，该方法包括以下步骤：1)将Y树脂，分别与X、Linker、Fmoc‑Leu‑OH偶联，得到Fmoc‑Leu‑Linker‑X‑Y树脂，其中X选自N端H由Dmb/Hmb/Tmb保护的氨基酸或Pro；2)在Fmoc‑Leu‑Linker‑X‑Y树脂上通过固相偶联合成方法依次接入序列中相应的保护氨基酸或片段，制得普卡那肽线性肽树脂；3)普卡那肽线性肽树脂经裂解，得到线性普卡那肽，经环化，即得普卡那肽。通过采用Fmoc‑Leu‑Linker‑X‑Y树脂用于普卡那肽的制备中，有效抑制合成过程中的缩聚现象。

Description

PCT国内申请，说明书已公开。

Claims (8)

  1. PCT国内申请，权利要求书已公开。
CN202080003011.9A 2020-09-10 2020-09-10 一种普卡那肽的制备方法 Active CN114585636B (zh)

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PCT/CN2020/114383 WO2022051963A1 (zh) 2020-09-10 2020-09-10 一种普卡那肽的制备方法

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CN114585636A true CN114585636A (zh) 2022-06-03
CN114585636B CN114585636B (zh) 2023-05-16

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107383171A (zh) * 2017-08-15 2017-11-24 苏州科技大学 一种通过二次环化固相合成普卡那肽的方法
CN108440652A (zh) * 2018-04-02 2018-08-24 杭州固拓生物科技有限公司 一种普卡那肽的固相合成方法
WO2018205401A1 (zh) * 2017-05-10 2018-11-15 深圳翰宇药业股份有限公司 一种普利卡那肽的制备方法
CN110903350A (zh) * 2019-12-27 2020-03-24 四川科伦药物研究院有限公司 一种普卡那肽的固相合成方法
WO2020115566A1 (en) * 2018-12-08 2020-06-11 Enzene Biosciences Limited An improved process for the preparation of plecanatide

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018205401A1 (zh) * 2017-05-10 2018-11-15 深圳翰宇药业股份有限公司 一种普利卡那肽的制备方法
CN107383171A (zh) * 2017-08-15 2017-11-24 苏州科技大学 一种通过二次环化固相合成普卡那肽的方法
CN108440652A (zh) * 2018-04-02 2018-08-24 杭州固拓生物科技有限公司 一种普卡那肽的固相合成方法
WO2020115566A1 (en) * 2018-12-08 2020-06-11 Enzene Biosciences Limited An improved process for the preparation of plecanatide
CN110903350A (zh) * 2019-12-27 2020-03-24 四川科伦药物研究院有限公司 一种普卡那肽的固相合成方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LI， H.D.等: "Liquid-Phase Total Synthesis of Plecanatide Aided by Diphenylphosphinyloxyl Diphenyl Ketone (DDK) Derivatives.", 《ORG. LETT.》 *

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CN114585636B (zh) 2023-05-16
WO2022051963A1 (zh) 2022-03-17

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