Solid phase polypeptide synthesis preparation method for leuprorelin

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 ...