| 摘要 |
<p>PURPOSE:To obtain human insulin useful as a remedy for diabetes, by eliminating protecting groups of a specific insulin derivative wherein arginine at a specific position is modified with a protecting group. CONSTITUTION:Protecting groups of insulin derivative shown by formula I (R<1> is OH-protecting group; R<2> is COOH-protecting group; R<3> is guanidiono- protecting group) wherein arginite at the 22-position of chain B is modified with a protecting group are eliminated, for example, R<3> [e.g., N<7>,N<8>-(1,2- dihydroxycyclohexylene-1,2)group(DHCH, for short), etc.,] is eliminated by allowing the derivative to stand in the presence of 1M hydroxyamine (pH 7) at 37 deg.C for 24hr and R<1> and R<2> (e.g., t-butyl group, etc.,) are eliminated by treating the derivative with trifluoroacetic acid in the presence of a cationic scavenger, to give the aimed substance, The compound shown by the formula I can be obtained by condensing [B22-Arg(DHCH)]des-B30-insulin shown by formula II derived from swine with an L-threonine derivative shown by formula III in the presence of an anzyme such as trypsin, etc.</p> |
