Preparation method of teriparatide
A technology of teriparatide and peptide resin, which is applied in the field of preparation of teriparatide, can solve the problems of unsuitability for large-scale production, low synthesis purity, and high cost, so as to reduce the difficulty of HPLC purification, optimize the synthesis process, and use safely Effect
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Embodiment 1
[0034] (1) Preparation of Fmoc-Phe-resin:
[0035] Take 0.1mol DIEA and 20g N, N-diisopropylcarbodiimide / 4-dimethylaminopyridine dual-system coupling reagent, join in the reaction vessel containing 0.6mol 2-CTC resin, then add 0.3molFmoc- Phe-OH carries out coupling reaction to obtain Fmoc-Phe-resin;
[0036] (2) Preparation of teriparatide-resin complex:
[0037]Add the mixture of triethylamine and DMF to the Fmoc-Phe-resin at a ratio of 1:2, stir to allow it to react for 30 minutes, then remove the liquid, wash the product 6 times with DMF, and wash it with N,N-DMF after the reaction After washing, the Phe-resin was obtained, and then 50 ml of the prepared 1:1:1 TBTU / HOBT / DIEA mixture was added, and the amino acids were extended and coupled one by one according to the order of teriparatide from the C-terminus to the N-terminus. The corresponding peptide resin was obtained after the second extension coupling, and after 120 minutes of coupling reaction, the teriparatide-resi...
Embodiment 2
[0046] (1) Preparation of Fmoc-Phe-resin:
[0047] Take 0.15molTEA and 25gN, N-diisopropylcarbodiimide / 4-dimethylaminopyridine dual-system coupling reagent, add to the reaction vessel filled with 0.75mol of 2-CTC resin, then add 0.5molFmoc- Phe-OH carries out coupling reaction to obtain Fmoc-Phe-resin;
[0048] (2) Preparation of teriparatide-resin complex:
[0049] Add the mixture of triethylamine and DMF to the Fmoc-Phe-resin at a ratio of 1:3.5, stir to allow it to react for 40 minutes, then remove the liquid, wash the product 6 times with DMF, and wash it with N,N-DMF after the reaction After washing, the Phe-resin was obtained, and then 60ml of 1:1:1 TBTU / Cl-HOBT / DIEA mixture was added, and the amino acids were extended and coupled one by one according to the order of teriparatide from C-terminal to N-terminal , the corresponding peptide resin was obtained after each extension coupling, and after 120 minutes of coupling reaction, the teriparatide-resin was obtained;
...
Embodiment 3
[0058] (1) Preparation of Fmoc-Phe-resin:
[0059] Take 0.2molDBU and 15gN, N-diisopropylcarbodiimide / 4-dimethylaminopyridine dual system coupling reagent, join in the reaction container that fills the 2-CTC resin of 0.55mol, then add 0.3molFmoc- Phe-OH carries out coupling reaction to obtain Fmoc-Phe-resin;
[0060] (2) Preparation of teriparatide-resin complex:
[0061] Add the mixture of triethylamine and DMF to the Fmoc-Phe-resin at a ratio of 1:4.5, stir to allow it to react for 30 minutes, then remove the liquid, wash the product 6 times with DMF, and wash it with N,N-DMF after the reaction After washing, the Phe-resin was obtained, and then 50 ml of the prepared 1:1:1 TBTU / HOBT / DIEA mixture was added, and the amino acids were extended and coupled one by one according to the order of teriparatide from the C-terminus to the N-terminus. The corresponding peptide resin was obtained after the second extension coupling, and after 120 minutes of coupling reaction, the teripa...
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