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1. WO2020107879 - SYNTHESIS METHOD FOR TERLIPRESSIN

Publication Number WO/2020/107879
Publication Date 04.06.2020
International Application No. PCT/CN2019/092743
International Filing Date 25.06.2019
IPC
C07K 7/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04Linear peptides containing only normal peptide links
16Oxytocins; Vasopressins; Related peptides
C07K 1/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
06using protecting groups or activating agents
C07K 1/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
06using protecting groups or activating agents
08using activating agents
CPC
C07K 1/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
02in solution
C07K 1/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
06using protecting groups or activating agents
C07K 1/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
06using protecting groups or activating agents
08using activating agents
C07K 7/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04Linear peptides containing only normal peptide links
16Oxytocins; Vasopressins; Related peptides
Applicants
  • 深圳翰宇药业股份有限公司 HYBIO PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 陈友金 CHEN, Youjin
  • 宓鹏程 MI, Pengcheng
  • 陶安进 TAO, Anjin
  • 袁建成 YUAN, Jiancheng
Agents
  • 深圳市深佳知识产权代理事务所(普通合伙) SHENPAT INTELLECTUAL PROPERTY AGENCY
Priority Data
201811438164.727.11.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) SYNTHESIS METHOD FOR TERLIPRESSIN
(FR) PROCÉDÉ DE SYNTHÈSE DE TERLIPRESSINE
(ZH) 一种特利加压素的合成方法
Abstract
(EN)
A synthesis method for terlipressin, wherein a compound Boc-Gly-Gly-Gly-active ester (3), a compound Boc-Cys-Pro-Lys-Gly-NH 2 (8) and a compound Boc-Tyr-Phe-Gln-Asn-active ester (13) are synthesized in segments using the liquid phase method, a compound (14) is obtained by connecting the compound (13) with the compound (8), a compound (15) is obtained after coupling the compound (14) with Boc-Cys(trt)-OH and deprotecting same, a compound (16) is obtained by connecting the compound (15) with the compound (3), and terlipressin is obtained by means of the oxidation of the compound (16).
(FR)
L'invention concerne un procédé de synthèse de terlipressine, un composé Boc-Gly-Gly-Gly-Ester actif (3), un composé Boc-Cys-Pro-Lys-Gly-NH 2 (8) et un composé Boc-Tyr-Phe-Gln-Asn-Ester actif (13) étant synthétisés en segments à l'aide du procédé en phase liquide, un composé (14) étant obtenu par liaison du composé (13) avec le composé (8), un composé (15) étant obtenu après couplage du composé (14) avec Boc-Cys (trt)-OH et déprotection de celui-ci, un composé (16) étant obtenu par liaison du composé (15) avec le composé (3), et la terlipressine étant obtenue au moyen d'une oxydation du composé (16).
(ZH)
一种特利加压素的合成方法,采用液相分片段合成化合物Boc-Gly-Gly-Gly-活性酯(3)、化合物Boc-Cys-Pro-Lys-Gly-NH 2 (8)和化合物Boc-Tyr-Phe-Gln-Asn-活性酯(13),化合物(13) 和化合物(8)连接得到化合物(14),化合物(14) 与Boc-Cys(trt)-OH 偶联脱保护后得到化合物(15),化合物(15) 和化合物(3) 连接得到化合物(16),化合物(16) 氧化得到特利加压素。
Also published as
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