Preparation method of antitumor small peptides FpAT

Abstract

The invention relates to a preparation method of antitumor small peptides FpAT. A technical scheme is characterized in that the preparation method comprises the following steps: adopting Fmoc / tBu solid-phase peptide synthesis technique and adopting 2-chlorotrityl chloride resin (CTC Resin) as a carrier to prepare Fmoc-Arg(Pbf)-CTC Resin having a substitutivity of 0.4-0.7mmol / g; sequentially condensing Fmoc protected amino acids having a sequence from the C-terminal to the N-terminal of FpAT through the solid-phase peptide synthesis technique until the condensation of the N-terminated aspartic acid is completed to obtain an FpAT fully-protected peptide resin; obtaining crude FpAT peptides through using a TFA / thioanisole / EDT / anisole as a cracking reagent and settling with anhydrous ether; and adding water to the crude FpAT peptides for dissolving, adjusting the pH value to 3-4, purifying through using preparative reverse phase HPLC, collecting a target product having a qualified purify, and lyophilizing to obtain the finished antitumor small peptides FpAT. The preparation method has the advantages of simple operation, high production efficiency, low equipment requirement, total yield reaching above 35%, realization of the large-scale production, and good economic and social values and application prospect.

Description

technical field [0001] The invention relates to the field of chemical synthesis of polypeptide drugs, in particular to a preparation method of the anti-tumor small peptide FpAT. Background technique [0002] The amino acid sequence of the anti-tumor small peptide FpAT is: L-aspartyl-L-seryl-glycyl-L-glutamyl-glycyl-L-aspartyl-L-phenylalanyl -L-Leucyl-L-Alanyl-L-Glutamyl-Glycyl-Glycyl-Glycyl-L-Valyl-L-Arginine. [0003] Its structure is as follows: [0004] [0005] Tumor is one of the most serious diseases that endanger human life and health. At present, there are many methods for treating tumors, such as surgery, radiotherapy, chemotherapy, etc., and tumor blood vessel blocking therapy. Among them, the anti-angiogenesis therapy developed based on the relationship between angiogenesis and tumor growth and metastasis is a relatively promising method, which provides hope for the treatment of cancer. Relevant studies have shown that the research on endogenous small anti-t...

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Problems solved by technology

[0007] Although patent 200610113568.X and WO2008040190A1 disclose a preparation method of FpAT small peptide, this method does not disclose the key materials (such as catalyst, reaction medium, etc.) or key reaction conditions involved in the reaction in the production method, which belongs to the synthesis of peptide drugs general method, it is difficult for those skilled in the art to prepare high-purity compounds in large quantities according to the disclosed content of the method

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