Method for preparing Nesiritide
A technology of crude peptide and resin, which is applied in the field of solid phase-liquid phase preparation, can solve the problems of unfavorable nesiritide industrial application, low yield of nesiritide, large environmental pollution, etc., and achieve considerable economic and practical value, future Ease of handling and less input of raw materials
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Embodiment 1
[0025] Embodiment 1: Preparation of Fmoc-His(Trt)-HMPB-AM resin
[0026] Add 7.2 g of HMPB-AM resin, with a substitution degree of 1.1 mmol / g, into a solid-phase reaction column, wash once with DMF, and swell the resin with DCM for 30 minutes, add 4.9 g of Fmoc-His(Trt)-OH, Add it to the above-mentioned reaction column equipped with resin and react for 2 hours. In order to improve the reaction efficiency, you can choose to add DIEA5-15ml. After the reaction was completed, it was washed 3 times with DMF and 3 times with DCM, blocked with methanol for 30 minutes, and then shrunk with methanol to obtain Fmoc-His(Trt)-HMPB-AM resin. The degree of substitution was 0.19 mmol / g.
Embodiment 2
[0027] Example 2: Preparation of side chain fully protected nesiritide-HMPB-AM resin
[0028] Weigh 20 g of Fmoc-His(Trt)-HMPB-AM resin (0.19 mmol / g, 3.8 mmol) into the reactor, wash once with DMF, and swell with DCM for 0.5 hours. After swelling, 20% DBLK was used to remove Fmoc protection, and then washed 4 times with DMF and 2 times with DCM. Dissolve 6.16g Fmoc-Arg(pbf)-OH (9.5mmol), 1.5g HOBt (11.4mmol), 1.8g DIC (14.3mmol) in DCM (a small amount of DMF can be added to aid dissolution), and add it to the solid phase reactor , and react at room temperature for 2h (the end point of the reaction is determined by the ninhydrin method). Repeat the above steps to complete Fmoc-Arg(Pbf)-OH, Fmoc-Leu-OH, Fmoc-Val-OH, Fmoc-Lys(Boc)-OH, Fmoc-Cys(Trt)-OH, Fmoc-Gly-OH , Fmoc-Leu-OH, Fmoc-Gly-OH, Fmoc-Ser(tBu)-OH, Fmoc-Ser(tBu)-OH, Fmoc-Ser(tBu)-OH, Fmoc-Ser(tBu)-OH, Fmoc -Ile-OH, Fmoc-Arg(Pbf)-OH, Fmoc-Asp(OtBu)-OH, Fmoc-Met-OH, Fmoc-Lys(Boc)-OH, Fmoc-Arg(Pbf)-OH, Fmoc-Gly -OH, F...
Embodiment 3
[0029] Example 3: Scale preparation of Nesiritide-HMPB-AM resin with fully protected side chains
[0030] Weigh 825g of Fmoc-His(Trt)-HMPB-AM resin (0.19mmol / g, 156.8mmol) into the reactor, wash once with DMF, and swell with DCM for 0.5 hours. After swelling, 20% DBLK was used to remove Fmoc protection, and then washed 4 times with DMF and 2 times with DCM. Dissolve 254.3g Fmoc-Arg(pbf)-OH (392mmol), 63.5g HOBt (470.4mmol), 74.3g DIC (588mmol) in DCM (a small amount of DMF can be added to aid dissolution), add to the solid phase reactor, room temperature Reaction for 2h (the end point of the reaction is determined by the ninhydrin method). Repeat the above steps to complete Fmoc-Arg(Pbf)-OH, Fmoc-Leu-OH, Fmoc-Val-OH, Fmoc-Lys(Boc)-OH, Fmoc-Cys(Trt)-OH, Fmoc-Gly-OH , Fmoc-Leu-OH, Fmoc-Gly-OH, Fmoc-Ser(tBu)-OH, Fmoc-Ser(tBu)-OH, Fmoc-Ser(tBu)-OH, Fmoc-Ser(tBu)-OH, Fmoc -Ile-OH, Fmoc-Arg(Pbf)-OH, Fmoc-Asp(OtBu)-OH, Fmoc-Met-OH, Fmoc-Lys(Boc)-OH, Fmoc-Arg(Pbf)-OH, Fmoc-Gly -OH...
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