| 摘要 |
A process for converting insulin compounds containing the human insulin moiety <IMAGE> into h-In-ThrB30 esters through transpeptidation of such insulin compounds with a threonine ester in solution of water and a water miscible solvent in the presence of trypsin and optionally an acid. Yields in excess of 60% are obtained by limiting water content to less than 50% v/v of the reaction mixture and controlling reaction temperature, with below ambient temperature and extended reaction times being preferred. A preferred starting material is the crude porcine insulin recovered from insulin salt cake and contaminated by proinsulin and degradation products thereof which contaminants convert into the h-In-ThrB30 ester.
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