Synthesis and in vitro evaluation of [18 F](R)-FEPAQ: a potential PET ligand for VEGFR2

J Prabhakaran, V Arango, VJ Majo, NR Simpson…

Index: Prabhakaran, Jaya; Arango, Victoria; Majo, Vattoly J.; Simpson, Norman R.; Kassir, Suham A.; Underwood, Mark D.; Polavarapu, Hanish; Bruce, Jeffrey N.; Canoll, Peter; John Mann; Dileep Kumar Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 5104 - 5107

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Citation Number: 5

Abstract

Synthesis and in vitro evaluation of [18F](R)-N-(4-bromo-2-fluorophenyl)-7-((1-(2-fluoroethyl) piperidin-3-yl) methoxy)-6-methoxyquinazolin-4-amine ((R)-[18F] FEPAQ or [18F] 1), a potential imaging agent for the VEGFR2, using phosphor image autoradiography are described. Synthesis of 2, the desfluoroethyl precursor for (R)-FEPAQ was achieved from t- butyl 3-(hydroxymethyl) piperidine-1-carboxylate (3) in five steps and in 50% yield.[18F] 1 ...