Synthesis of new carbon-11 labeled cyclofenil derivatives for PET imaging of breast cancer estrogen receptors.
Carbon-11 labeled cyclofenil derivatives, [(11)C]methyl-2-{4-[bis(4-hydroxyphenyl)methylene]cyclohexyl}acetate ([(11)C]16a), [(11)C]methyl-4-[bis(4-hydroxyphenyl)methylene]cyclohexanecarboxylate ([(11)C]16b), [(11)C]methyl-2-{3-[bis(4-hydroxyphenyl)methylene]cyclohexyl}acetate ([(11)C]18a), and [(11)C]methyl-3-[bis(4-hydroxyphenyl)methylene]cyclohexanecarboxylate ([(11)C]18b), have been synthesized as new potential PET agents for imaging breast cancer estrogen receptors. The target tracers were prepared by O-[(11)C]methylation of their corresponding precursors using [(11)C]CH(3)OTf and isolated by a simplified SPE purification procedure in 35-50% radiochemical yields decay corrected to EOB, 15-20 min overall synthesis time, and 74-111 GBq/micromol specific activity at EOS.
D001943:Breast Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000737:chemistry*; D003506:Cyclofenil / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D005260:Female; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D011960:Receptors, Estrogen / Q000032:analysis* / Q000096:biosynthesis
D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D011960:Receptors, Estrogen; D003506:Cyclofenil