Synthesis of carbon-11-labeled bivalent β-carbolines as new PET agents for imaging of cholinesterase in Alzheimer's disease.
Carbon-11-labeled bivalent β-carbolines, 9,9'-(pentane-1,5-diyl)bis(2-[(11)C]methyl-9H-pyrido[3,4-b]indol-2-ium)iodide ([(11)C]2a), 9,9'-(nonane-1,9-diyl)bis(2-[(11)C]methyl-9H-pyrido[3,4-b]indol-2-ium)iodide ([(11)C]2b), 9,9'-(dodecane-1,12-diyl)bis(2-[(11)C]methyl-9H-pyrido[3,4-b]indol-2-ium)iodide ([(11)C]2c) and 1,9-bis(2-[(11)C]methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-9(2H)-yl)nonane ([(11)C]3), were prepared by N-[(11)C]methylation of their corresponding amine precursors using [(11)C]CH(3)I and isolated by either a simplified solid-phase extraction (SPE) method or HPLC in 40-60% radiochemical yields based on [(11)C]CO(2) and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 20-30min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 185-370 GBq/μmol.
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, 46202, USA.
Min
M
Wang
David X
DX
Zheng
Mingzhang
M
Gao
Gary D
GD
Hutchins
Qi-Huang
QH
Zheng
D000544:Alzheimer Disease / Q000000981:diagnostic imaging / Q000201:enzymology*; D002243:Carbolines / Q000138:chemical synthesis* / Q000737:chemistry; D002250:Carbon Radioisotopes / Q000737:chemistry*; D002802:Cholinesterases / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D049268:Positron-Emission Tomography
D002243:Carbolines; D002250:Carbon Radioisotopes; D002802:Cholinesterases