SYNTHESIS, ATTEMPTED KINETIC RESOLUTION AND EVALUATION OF [I-123] MK-447 ANALOGS AS INFLAMMATION RADIOPHARMACEUTICALS

The non-steroidal anti-inflammatory agent 2-amino-methyl-4-tert-butyl- 6-iodophenol hydrochloride (MK-447) and some of its analogues were lab elled with I-123 and tested in an inflamed rat-paw model. Even though MK-447 has a significant anti-inflammatory activity, and a 2.3 ratio f or inflamed site over muscle, its usefullness for scintigraphic detect ion of inflammation is hindered by its high uptake in the skin. The ki netic resolution of diastereomeric products with chiral dienyl iron co mplexes was unsuccessful as the signals from the respective H-1 and C- 13 NMR spectra were coincident.