On the power of super acid-lodieatioe of aromatic ring in the presence of imidazole moiety of the potent gamma secretase modulators (GSM) en route to tritium labeling

摘要

Two advanced leads from the GSM program were iodinated selectively on the aromatic ring in the presence of an imidazole fragment using Olah's reagent-the combination of NIS and trifluoromethanesulfo-nic acid. These iodinated compounds were tritium labeled via a transition metal catalyzed sodium borotritide reduction for the purpose of metabolite studies.