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Solid phase polypeptide synthesis preparation method for leuprorelin

A solid-phase peptide synthesis, leuprolide technology, applied in the preparation methods of peptides, chemical instruments and methods, peptides and other directions, can solve the limitations of large-scale production and use of leuprolide acetate, low peptide yield, The problem of high production cost, to achieve the effect of low production cost, high yield and less three wastes

Active Publication Date: 2006-11-22
SHANGHAI SOHO YIMING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There are certain defects in the current methods. Trifluoroacetic acid must be used for each round of decapping, so the peptide yield is low, resulting in high production costs; there are many wastes, and trifluoroacetic acid is used for purification, which pollutes the environment. The rate is generally below 25%
Therefore current methods limit the large-scale production and use of leuprolide acetate

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

Shanghai Chemical Reagent Company

[0093] In the example:

[0094] Said peptide-connecting reagent is: NMM:DMF=1:10, volume ratio;

[0095] Said decapping reagent is: PIP: DMF=1: 3.5, volume ratio;

[0096] synthetic peptide chain

[0097] Preparation of Fmoc-Pro-Wang resin

[0098] 1) Take 75g of Wang resin (0.8mmol / g resin, 60mmol), soak in 1000ml of DMF to fully swell the resin, and blow dry.

[0099] 2) Take 81g (FW: 337.4, 240mmol) Fmoc-Pro-OH, 77.1g (FW: 321, 240mmol) TBTU / HBTU, 36.6g (FW: 153, 240mmol) HOBT, dissolve it with 750ml peptide reagent, add to the reaction Container, react at 25°C for 1 hour.

[0100] 3) Blow dry, wash with DMF, absolute ethanol and DMF respectively three times, and blow dry to obtain about 85g.

[0101] Preparation of Fmoc-Arg(Pbf)-Pro-Wang resin:

[0102] 1) Add 1000ml decapping reagent, react at 25°C for 15 minutes, blow dry, wash with DMF, absolute ethanol and DMF respectively three times, and blow dry.

[0103] 2) Add 155....

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PUM

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Abstract

The invention discloses a bright-ala-ruilin preparing method of solid-phase polypeptide, which comprises the following steps: adopting Wang resin or CTC resin as original material to connect amino with protective group to produce protective nonapeptide resin; removing Fmoc-protective group sequently; proceeding side-chain protective group synchronizingly and cutting peptide; connecting ethylamine through ethylamine-to-HOBT to produce crude product; proceeding separation and purifying through C18 (or C8) pillar to produce fine bright-ala-ruilin. The invention avoids the utility of poisonous agent, which improves the purifying, peptide connecting and obtaining rate.

Description

technical field [0001] The invention relates to a preparation method of leuprolide, in particular to a preparation method of solid-phase polypeptide synthesis of leuprolide. Background technique [0002] Leuprorelin, the Chinese name is Leuprorelin acetate, or other names for short: Leuprorelin, the English name is Leuprorelin, and the structural formula is pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro -NHC 2 h 5 , formula C 59 h 84 N 16 o 12 ·C 2 h 4 o 2 , the molecular weight is 1269.48. [0003] Leuprolide is clinically used to treat related hormone disorders, including advanced prostate cancer, endometriosis, central precocious puberty, etc. [0004] Leuprolide acetate is a gonadotropin-releasing hormone analog, which mainly acts on the anterior lobe of the pituitary gland. In the early stage of high-dose application, it can cause a transient increase in the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It leads to decreased sensitivity ...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K1/04
CPCY02P20/55
Inventor 周达明
Owner SHANGHAI SOHO YIMING PHARMA
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