Process for preparing human insulin or b-30 esters thereof

C - Chemistry – Metallurgy – 12 – P

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195/128.2

C12P 21/02 (2006.01) C07K 14/62 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1174623

Abstract Human insulin or B-30 esters thereof are prepared by reacting an insulin derivative of the formula Image (I) wherein R is hydroxyl or an amino acid radical being different from threonine, and -A- and -B- represent the A- and B-chains with the same amino acid sequence as in human insulin, with a carboxyl protected and optionally hydroxyl protected L-threonine derivative in a concentration of from 2.5 to about 6 moles per litre in the presence of trypsin or a trypsin-like enzyme in a reaction medium containing water and optionally also an organic cosolvent at a pH value of from 5 to 9 and at a temperature below 50°C., followed, if desired, by removal of any protecting groups present. Human insulin is prepared in an easy and simple way in high yield and in high purity.

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