Collect. Czech. Chem. Commun. 1988, 53, 2936-2943

Synthesis of [3H-TyrB26]-human insulin by enzymic semisynthesis

André Hänsickea, Michael Beyermannb, Johannes Oehlkeb, Erhard Mittagc, Uwe Kertscherb, Zhanna D. Bespalovad, Mikhail I. Titovd, Michael Bienertb, Klaus-Dieter Kaufmanna and Hartmut Niedrichb

a VEB Berlin-Chemie, Glienicker Weg 124, Berlin, G.D.R. – 1199
b Institute of Drug Research, Academy of Sciences of G.D.R., Alfred-Kowalke-Str. 4, Berlin, G.O.R. – 1136
c Central Institute of Nuclear Research, Rossendorf, G.D.R.
d USSR Cardiological Research Centre, Academy of Medical Sciences, 121500 Moscow, 3rd Cherepkovskaya ulitsa, U.S.S.R.


A procedure is described for tritium labeling of human insulin in position TyrB26 by means of trypsin catalyzed condensation of DiBoc-DOI with [Nε-Boc, 3H-TyrB26]-IOP, subsequent deprotection and purification by HPLC. The tritium labeling of the octapeptide was accomplished by dehalotritiation of the corresponding DitB26-octapeptide which was obtained both by iodination of Nε-Boc-IOP and by total synthesis.