Initial PET studies in rats with novel radiotracer [11C]D617 and comparison with (R)-[11C]verapamil

The aim of this study is to develop the synthesis of [11C]D617 and to study its brain distribution in rats with and without pre-treatment with P-gp inhibitor tariquidar and compare the results with previous data obtained with (R)-[11C]verapamil. The precursor for labelling D617 with C-11, compound 5, was synthesized in 4 steps and subsequently reacted with [11C]methyl triflate to give [11C]D617. a: DMF, NaH, isopropyl bromide, RT, 5h, 77%; b: THF, n-BuLi, 1,3-dibromopropane -78°C, 2h, 83%; c: toluene, 18-Crown-6, potassium phtalimide, reflux 6h, 86%; d: THF, EtOH, hydrazine.H2O, RT, 2h, 74%; e: methylamine, toluene/H2O, 56%.