Preparation method of Bivalirudin

A technology of bifarudine and peptide resin, applied in the field of peptide solid-phase synthesis, can solve the problems of complicated operation and many impurities.

Active Publication Date: 2010-12-08
SHANGHAI AMBIOPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

US20090062511A discloses a method for solid-phase synthesis of bivalirudin, which uses a solid-phase synthesis method, which is cumbersome to operate and produces many impurities

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  • Preparation method of Bivalirudin
  • Preparation method of Bivalirudin
  • Preparation method of Bivalirudin

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Abstract

The invention discloses a preparation method of polypeptide solid-phase synthesis Bivalirudin, comprising the following steps of: (1) condensing Fmoc-Asn(Trt)-Gly-OH with a polypeptide resin shown as the formula V in the presence of a condensing agent to obtain a polypeptide resin shown as the formula III; (2) mixing the polypeptide resin shown as the formula III with a deprotection agent to remove a Fmoc protective group; (3) condensing Fmoc-Gly-Gly-Gly-Gly-OH with a polypeptide resin shown as the formula VI in the presence of the condensing agent to obtain a polypeptide resin shown as the formula IV; (4) sequentially condensing polypeptide of the polypeptide resin shown as the formula IV with amino acids from the end C to the end N according to the sequence from Pro to Arg, Pro and to D-Phe by a method of solid-phase synthesis so as to prepare a polypeptide resin shown as the formula II; and (5) separating polypeptide and resin on the polypeptide resin shown as the formula II in thepresence of a separating agent to obtain Bivalirudin shown as the formula I.

Description

technical field The invention relates to the field of polypeptide solid-phase synthesis, in particular to a solid-phase synthesis method for Bivalirudin. Background technique It was R. Bruce Merrifield who made a breakthrough in the technology of peptide synthesis. He designed a peptide synthesis pathway and named it the solid-phase synthesis pathway. First, an amino acid whose amino group is protected by a blocking group is covalently linked to a solid-phase support; under the action of a deprotecting agent, the amino-protecting group is removed, so that the first amino acid is connected to the solid-phase support. Then the carboxyl group of the second amino acid whose amino group is blocked is activated by a reagent, and the second amino acid whose carboxyl group is activated by DCC reacts with the amino group of the first amino acid that has been attached to the solid-phase carrier to form a peptide bond, so that on the solid-phase carrier A dipeptide with a protecting g...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K1/06C07K1/04
CPCC07K14/815Y02P20/55
Inventor 白俊才张若平刘亚东张国庆
Owner SHANGHAI AMBIOPHARM
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