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. 2014 Sep 9;57(19):7999–8009. doi: 10.1021/jm500872p

Scheme 1. Synthesis of 6, Its Radiolabeling Precursor (4) and [11C]6.

Scheme 1

Reagents and conditions: (a) NaBH4, MeOH, overnight, rt, 75%; (b) formaldehyde, AcOH, NaBH4, MeOH, rt, overnight, 55%. (c) NH2OH (aq), 1M NaOH, MeOH/THF, 0 °C to rt, 4 h, 42% for 6, 40% for 5; RCY of [11C]6, 3–5% (non-decay corrected to trapped [11C]CH3I).