Thymopetidum acetyl methyl ester conjugate (FPSDM-TP5) and preparation method thereof
The invention relates to a thymopetidum acetyl methyl ester conjugate (FPSDM-TP5) and a preparation method thereof. The preparation method comprises the following steps of: dissolving Z-FPSDM-Arg(Pbf)-OH and 1-hydroxy-1H-1,2,3-triazole-4-carboxylic acid ethyl ester in anhydrous dichloromethane, addi...
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Zusammenfassung: | The invention relates to a thymopetidum acetyl methyl ester conjugate (FPSDM-TP5) and a preparation method thereof. The preparation method comprises the following steps of: dissolving Z-FPSDM-Arg(Pbf)-OH and 1-hydroxy-1H-1,2,3-triazole-4-carboxylic acid ethyl ester in anhydrous dichloromethane, adding N,N-diisopropyl carbodiimide with stirring, and reacting to obtain active ester A; dripping the active ester A into an alkaline solution of a tetrapeptide derivative, adding N-diisopropylethylamine, stirring for complete reaction, adding dichloromethane, and thus obtaining a crude thymopetidum acetyl methyl ester conjugate product; and adding trifluoroacetic acid, stirring, distilling under reduced pressure to extract the trifluoroacetic acid completely so as to obtain residues, and washing and drying the residues in turn to obtain the thymopetidum acetyl methyl ester conjugate. The FPSDM-TP5 slows down or avoids the enzymolysis of TP5 in vivo while keeping the bioactivity of the TP5, so that the metabolic half-life of the TP5 in vivo is obviously prolonged. |
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