Synthesis of new carbon-11 labeled naphthalene-sulfonamides for PET imaging of human CCR8.
Carbon-11 labeled naphthalene-sulfonamides, N-(4-(N-(4-[(11)C]methoxyphenyl)sulfamoyl)naphthalene-1-yl)benzamide ([(11)C]5a), N-(4-(N-(4-[(11)C]methoxyphenyl)sulfamoyl)naphthalene-1-yl)-2-methylbenzamide ([(11)C]5b), N-(4-(N-(4-[(11)C]methoxyphenyl)sulfamoyl)naphthalene-1-yl)-3-methylbenzamide ([(11)C]5c), N-[(11)C]methyl-N-methyl-4-(4-benzamidonaphthalene-1-sulfonamido)piperidine-1-carboxamide ([(11)C]9a) and N-[(11)C]methyl-N-methyl-4-(4-(2-methylbenzamido)naphthalene-1-sulfonamido)piperidine-1-carboxamide ([(11)C]9b), have been synthesized as new potential positron emission tomography (PET) agents for imaging of human CCR8. The target tracers were prepared by either O-[(11)C]methylation or N-[(11)C]methylation of their corresponding precursors using [(11)C]CH(3)OTf and isolated by either a simplified solid-phase extraction (SPE) purification procedure or a high pressure liquid chromatography (HPLC) method in 30-50% radiochemical yields decay corrected to end of bombardment (EOB), 20-25 min overall synthesis time, and 74-111 GBq/micromol specific activity at end of synthesis (EOS).
Wang
Min
M
Department of Radiology, Indiana University School of Medicine, 1345 West 16th Street, L-3 Room 202, Indianapolis, IN 46202, USA.
Cooley
Benjamin
B
Gao
Mingzhang
M
Miller
Kathy D
KD
Sledge
George W
GW
Hutchins
Gary D
GD
Zheng
Qi-Huang
QH
D002250:Carbon Radioisotopes / Q000737:chemistry*; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000737:chemistry*; D054401:Receptors, CCR8 / Q000737:chemistry*; D013449:Sulfonamides / Q000737:chemistry*
C103330:CCR8 protein, human; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D054401:Receptors, CCR8; D013449:Sulfonamides