Abstract
Insulin and NαB1-trifluoroacetylinsulin were crosslinked by diaminodicarboxylic acids, preferably α,α′-diamino-suberic acid (Dsa), using bis-(tert-butyloxycarbonyl)-2.7-diaminosuberoyl-bis-(2.4.5-trichlorophenylate) [(BOC)2-Dsa-(OTcp)2] as coupling reagent. Elimination of the BOC groups by trifluoroacetic acid treatment and Edman degradation resulted in biologically fully active des-PheB1-insulin and NαB1-Tfa-insulin, respectively. The Nα group of the natural A-chain tetrasulfonate and the NɛB29 group of the natural B-chain disulfonate, specifically trifluoroacetylated in NαB1, were linked together by successive reaction with the above mentioned reagent. After formation of the correct disulfide bridges in high yields (60–75 %) the elimination of the connecting Dsa by Edman degradation yielded NαB1-Tfa-insulin, which was biologically fully active.
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