S. Landvatter
Sep 1, 1993
Citations
0
Influential Citations
3
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
The N2-methyl amino acid NG-mesitylenesulfonyl-[3H]methylarginine has been prepared in high specific activity tritium labelled form by treating methyl N2-2,4-dimethoxybenzyl-NG-mesitylenesulfonyl-arginate with [3H]methyl iodide and silver(I) oxide. Removal of the dimethoxybenzyl group by transfer hydrogenation (4.4% formic acid in methanol/Pd black) followed by saponification gave NG-mesitylenesulfonyl-[3H]methylarginine in 30-38% overall from [3H]methyl iodide. This amino acid was ultimately used in the preparation of tritium labelled SK&F 107260 which is a cyclic peptide showing fibrinogen receptor antagonism.