Method for preparing Eptifibatide with solid phase method
A technology of solid-phase method and solid-phase reaction, which is applied to peptide preparation methods, chemical instruments and methods, blood diseases, etc., can solve the problems of complex operation production cycle and low application value, and achieve considerable economic and practical value and low cost. Low, high yield effect
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Embodiment 1
[0036] Example 1 Preparation of Epifibatide Peptide Resin with Fully Protected Linear Side Chains
[0037]Add 100.0 g of Sieber resin, with a substitution degree of 0.6 mmol / g, into the solid-phase reaction column, and swell the resin with DMF for 30 minutes. After the swelling is complete, use 20% DBLK to remove Fmoc protection for 10min+20min, and then wash with DMF six times. Add 49.74g of Fmoc-Cys(Acm)-OH, 38.52g of HBTU, 16.2g of HOBt and 41.8ml of DIPEA into the reaction column, and the reaction is completed in two hours. Repeat the previous operation to couple Fmoc-Pro-OH, Fmoc-Trp-OH, Fmoc-Asp(OtBu)-OH, Fmoc-Gly-OH, Fmoc-Homoarg(pbf)-OH and Acm-Mpr-OH respectively couplet. After the coupling was completed, the resin was washed three times with DMF, three times with DCM, shrunk three times with methanol, and weighed after vacuum drying to obtain 172.1 g linear side chain fully protected Epifibatide peptide resin. Another preferred solution of this embodiment is: add ...
Embodiment 2
[0038] Example 2 Preparation of Epifibatide Peptide Resin with Fully Protected Oxidized Side Chains
[0039] 172.1 g of linear side chain fully protected Epifibatide peptide resin was swelled with DMF for 30 minutes. After the swelling is complete, 304.8g of iodine dissolved with an appropriate amount of DMF is added to the reaction column equipped with the resin, and the oxidation reaction is carried out for 2 hours. After the reaction was completed, it was washed ten times with DMF, three times with DCM, and shrunk three times with methanol. After vacuum drying, it was weighed to obtain 164.1 g of oxidized side chain fully protected Epifibatide peptide resin.
Embodiment 3
[0040] Example 3 Preparation of Epifibatide Peptide Resin with Fully Protected Oxidized Side Chains
[0041] 1893 g of linear side chain fully protected Epifibatide peptide resin was swelled with DMF for 30 minutes. After the swelling is complete, 3350g of iodine dissolved with an appropriate amount of DMF is added to the reaction column equipped with the resin, and the oxidation reaction is carried out for 3 hours. After the reaction was completed, it was washed ten times with DMF, three times with DCM, and shrunk three times with methanol. After vacuum drying, it was weighed to obtain 1740 g of fully protected Epifibatide peptide resin with oxidized side chains.
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