Journal of labelled compounds and radiopharmaceuticals p. 1239 - 1252 (2002)
Update date:2022-08-03
Topics:
Zheng, Qi-Huang
Liu, Xuan
Fei, Xiangshu
Wang, Ji-Quan
Ohannesian, David W.
Erickson, Leonard C.
Stone, K. Lee
Martinez, Tanya D.
Miller, Kathy D.
Hutchins, Gary D.
Novel radiolabeled O6-benzylguanine derivatives, 2-amino-6-O-[11C]-[(methoxymethyl)benzyloxy]-9-benzyl purines ([11C]p-O6AMBP, 1a; [11C]m-O6-AMBP, 1b; [11C]o-O6-AMBP, 1c), have been synthesized for evaluation as new potential positron emission tomography (PET) tumor imaging agents for the DNA repair protein, O6-alkylguanine-DNA alkyltransferase (AGT). The appropriate precursors for radiolabeling were obtained in three steps from starting material 2-amino-6-chloropurine with moderate to excellent chemical yields. Tracers were prepared by O-[11C]methylation of hydroxymethyl precursors using [11C]methyl triflate. Pure target compounds were isolated by solid-phase extraction (SPE) purification procedure in 45-60% radiochemical yields (decay corrected to the end of bombardment), and a synthesis time of 20-25 min. Copyright
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