Glucagon production method
A glucagon, C-terminal technology, applied in the field of glucagon manufacturing, can solve problems such as low glucagon purity
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example 1
[0182] Example 1. Synthesis of Boc-His(Trt)-Ser(tBu)-Gln(Trt)-Gly-OH
[0183]The synthesis of the title tetrapeptide was carried out by SPPS on CTC resin (2 g). After swelling the resin with DCM (20 mL), Fmoc-Gly-OH (1 eq for resin loading) and DIEA (2 eq) dissolved in DCM (12 mL) were added to the resin and allowed to react for 1 hour . Then, the resin was washed with DCM (3 x 12 mL), and the residual free chlorine groups were replaced with MeOH and DIEA in DCM. The residual hydroxyl groups were capped with 0.5 MAc2O in DCM (12 mL, 15 min) and washed with DCM (3 x 12 mL). Then, the resin was swelled with DMF (12 mL) for 30 minutes. The Fmoc group was removed by treatment with 20% piperidine in DMF (2 x 12 mL, 10 min each cycle) and washed with DMF (4 x 12 mL, 2 x 5 min and 2 x 10 min). Resin loading after insertion of the first amino acid was assessed by UV measurement of the deprotection solution at 301 nm, giving a loading of 1.2 mmol / g.
[0184] The next amino acids u...
example 2
[0187] Example 2. Preparation of Glucagon
[0188] Resin loading
[0189] Glucagon synthesis was carried out by SPPS on Wang's resin (3 g). After swelling the resin with DMF (10 mL), Fmoc-Thr(tBu)-OH (4 eq in terms of resin loading) was preactivated with DIC and DMAP (2 eq and 0.1 eq, respectively) in DMF (18 mL)5 minutes, it was then added to the resin and allowed to couple for 60 minutes. Then, the resin was washed with DMF (3×6 mL), and washed with 0.5M Ac 2 O in DMF (6 mL, 15 min) capped the remaining free hydroxyl groups and washed them with DMF (3 x 6 mL). The Fmoc group was removed by treatment with 20% piperidine in DMF (2 x 6 mL, 10 min each cycle) and washed with DMF (4 x 6 mL, 2 x 5 min and 2 x 10 min). Resin loading after insertion of the first amino acid was assessed by UV measurement of the deprotection solution at 301 nm, resulting in a loading of 0.7 mmol / g.
[0190] The resin thus obtained was divided into three fractions (1 g of starting resin each): on...
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