Synthesis and evaluation of novel tropane derivatives as potential PET imaging agents for the dopamine transporter

H Qiao, L Zhu, BP Lieberman, Z Zha, K Plössl…

Index: Qiao, Hongwen; Zhu, Lin; Lieberman, Brian P.; Zha, Zhihao; Ploessl, Karl; Kung, Hank F. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 13 p. 4303 - 4306

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Citation Number: 5

Abstract

A novel series of tropane derivatives containing a fluorinated tertiary amino or amide at the 2β position was synthesized, labeled with the positron-emitter fluorine-18 (t1/2= 109.8 min), and tested as potential in vivo dopamine transporter (DAT) imaging agents. The corresponding chlorinated analogs were prepared and employed as precursors for radiolabeling leading to the fluorine-18-labeled derivatives via a one-step nucleophilic ...