4 results about "MBHA resin" patented technology

The invention provides a synthesis method of natriuretic peptide GNP, which comprises the following steps: step S1: Fmoc-Nle, HMP link-OH and a solid phase carrier are coupled to obtain HMP link-Nle-MBHA Resin, the solid phase carrier is MBHA Resin resin, and the degree of substitution is 0.40 mmol / g to 0.62 mmol / g; step S2, connecting Fmoc-Arg (Pbf)-OH, so as to obtain Fmoc-Arg (Pbf)-HMPA Resin; s3, according to the sequence of the natriuretic peptide GNP, the Fmoc protecting group of each amino acid or fragment is removed, the amino acids or fragments are coupled one by one, Gly33-Asp34 adopts Fmoc-Asp (OtBu)-Gly-OH fragments, and natriuretic peptide GNP peptide resin is obtained; and S4, carrying out cleavage reaction and oxidation reaction on the natriuretic peptide GNP peptide resin to obtain a natriuretic peptide GNP crude product. By optimizing the chemical synthesis process and the cracking and oxidation process, the purity and yield of the crude product can be greatly improved, and the method has wide practical value and application prospect.

The invention relates to the technical field of polypeptide drugs, and provides a synthesis method of abparatide, which comprises the following steps: by taking Rink Amide AM resin, Rink MBHA resin or Rink Amide resin as a solid-phase carrier, sequentially coupling single amino acid and 19-21 tripeptide fragments or 19-22 tetrapeptide fragments from N terminal to C terminal through a solid-phase synthesis method according to a primary sequence of abparatide, so as to obtain abparatide peptide resin; the abparatide peptide resin is cracked to obtain abparatide, and a coupling agent / alkali adopted for coupling is selected from at least one of Oxyma / DIC, COMU / DIEA, COMU / TMP, PyOxim / DIEA and TPTU / DIEA. The abparatide crude peptide synthesized by the method disclosed by the invention is high in yield and high in purity, and the synthesis method disclosed by the invention shortens the production time, reduces the production cost and is beneficial to commercial production.

The invention provides a method for synthesizing tepote, comprising the steps of reacting Fmoc-Linker-OH, HBTU and swollen AM Resin to obtain Fmoc-Linker-AM Resin; adding Fmoc-Ser(tBu)-OH and HOBT to a reaction system of resin and PIP / DMF and reacting completely; coupling from the C-terminus to the N-terminus to obtain a fully protected peptide resin; adding a cleavage reagent to the fully protected peptide resin, reacting and collecting the filtrate, cooling and precipitating, and drying to obtain a crude peptide. The method solves the problem that the linker on the MBHA Resin in the prior art will break and generate new impurities; avoids the disadvantage of using heavy metal palladium or genotoxic substance hydrazine hydrate; solves the problem that the C-terminal Pro 36 、Pro 37 、Pro 38 The problem of [‑(Pro‑Pro)] missing impurities produced by step-by-step coupling is solved; the finished product is saved and is conducive to industrial production.

The invention belongs to the technical field of biomedical materials, and particularly relates to a targeted NPY polypeptide nuclide ligand as well as a preparation method and application thereof. The structural formula of the targeted NPY polypeptide nuclide ligand is as shown in formula (1), wherein L is a metal chelating agent. The preparation method comprises the following steps: (1) adding tyrosine, an activating agent, a condensing agent and a solvent into Rink Amide MBHA Resin, reacting at room temperature for 1-5 hours, and grafting tyrosine on the Rink Amide MBHA Resin; (2) adding arginine, an activating agent, a condensing agent and a solvent, reacting at room temperature for 1-5 hours, grafting arginine, and sequentially grafting glutamine, arginine, tryptophan, isoleucine, proline, asparagine, asparagine, tyrosine, histidine, arginine and a metal chelating agent according to the steps, so as to obtain polypeptide resin L-Arg-His-Tyr-Asp-Asp-Pro-Iso-Try-Arg-Gln-Arg-Tyr-Rink Amide MBHA Resin; and (3) adding the obtained polypeptide resin into a lysis solution, and reacting at room temperature for 1-5 hours to obtain the targeted NPY polypeptide nuclide ligand with good in-vivo and in-vitro stability.