Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Solid phase polypeptide synthesis preparation method for leuprorelin

A technology of solid-phase peptide synthesis and leuprolide, which is applied in the preparation method of peptides, chemical instruments and methods, peptides, etc., can solve the problems of three wastes pollution, high production cost, and environmental pollution.

Active Publication Date: 2012-03-21
SHANGHAI SOHO YIMING PHARMA
View PDF2 Cites 3 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] The list of raw materials adopted in the embodiment and the foregoing process is as follows:

[0092] no product name manufacturer 1 Wang Resin Tianjin Hecheng Technology Co., Ltd. 2 Fmoc-Pro-OH Sichuan Sangao Biochemical Co., Ltd. 3 Fmoc-Arg(Pbf)-OH Sichuan Sangao Biochemical Co., Ltd. 4 Fmoc-Leu-OH Sichuan Sangao Biochemical Co., Ltd. 5 Fmoc-D-Leu-OH Sichuan Sangao Biochemical Co., Ltd. 6 Fmoc-Tyr(tBu)-OH Sichuan Sangao Biochemical Co., Ltd. 7 Fmoc-Ser(tBu)-OH Sichuan Sangao Biochemical Co., Ltd. 8 Fmoc-Trp-OH Sichuan Sangao Biochemical Co., Ltd. 9 Fmoc-His(Trt)-OH Sichuan Sangao Biochemical Co., Ltd.

[0093] 10 p-Glu-OH Sichuan Sangao Biochemical Co., Ltd. 11 1-Hydroxybenzotriazole (HOBt) Sichuan Sangao Biochemical Co., Ltd. 12 TBTU Sichuan Sangao Biochemical Co., Ltd. 13 Trifluoroacetic acid (TFA) Merck 14 N-Methylmorpholine (NMM) Merc...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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 ethylaminethrough 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K1/04
CPCY02P20/55
Inventor 周达明
Owner SHANGHAI SOHO YIMING PHARMA
Features
  • Generate Ideas
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com