Synthesis method of high-purity leuprorelin

The invention provides a method for preparing leuprorelin. The method comprises the following steps: (1) taking Fmoc-Pro-CTC-OH and CTC (Carbon Tetrachloride) resin as starting raw materials and treating to obtain Fmoc-Pro-CTC-OH resin; (2) sequentially connecting the Fmoc-Pro-CTC-OH resin with an a...

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Bibliographische Detailangaben
Hauptverfasser: WANG LINPENG, LIU BING, SHAN LIANMIN, ZHANG DAOGUI, JIANG XIAOMAN, AN NING, WAN LONGYAN
Format: Patent
Sprache:chi ; eng
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Beschreibung
Zusammenfassung:The invention provides a method for preparing leuprorelin. The method comprises the following steps: (1) taking Fmoc-Pro-CTC-OH and CTC (Carbon Tetrachloride) resin as starting raw materials and treating to obtain Fmoc-Pro-CTC-OH resin; (2) sequentially connecting the Fmoc-Pro-CTC-OH resin with an amino acid with a protecting group by adopting a gradual coupling manner of a Fmoc/tBu solid-phase method to synthesize side chain wholly-protected leuprorelin precursor peptide-resin; (3) taking a 20 percent trifluoroethanol/DCM (Dichloromethane) solution as a cutting reagent and cutting the side chain wholly-protected leuprorelin precursor peptide-resin, so as to obtain a side chain wholly-protected leuprorelin precursor peptide; (4) carrying out ethyl amination on the side chain wholly-protected leuprorelin precursor peptide to obtain side chain wholly-protected leuprorelin; (5) carrying out side chain cutting on the side chain wholly-protected leuprorelin to obtain a leuprorelin crude peptide; (6) carrying out C