摘要 |
PURPOSE:To easily produce a human insuline ester in high conversion on an industrial scale at a low cost by a semi-synthetic means, by introducing threo nine group to a specific raw material in the presence of immobilized trypsin. CONSTITUTION:Swing insulin is digested with carboxypeptidase A to obtain a swine insulin (DAI) devoid of 30-site alanine group on the chain B. About 6mM of DAI is mixed with about 0.6M of oily tertbutoxythreonine, about 60% dimethylformamide-ethanol mixture (1:1V/V) and about 22wt% water and the mixture is adjusted to about 7pH and diluted to 100wt%. About 1ml of the liquid mixture is passed through e.g. a column filled with trypsin immobilized to spherical agarose, etc., at a flow rate of about 1ml/2.5hr at <=12 deg.C. The objective human insulin ester is produced in the reaction liquid by the above- semi-synthetic reaction.
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