Abstract
Carbon-11 labeled biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues, 2-(2-(biphenyl-4-yl)ethyl)-6-[ 11C]methoxy-7-methoxy-1,2,3,4-tetrahydroisoquinoline ([ 11C] 3); 1-(biphenyl-4-yl)methyl-6,7-dimethoxy-2-[ 11C]methyl-1,2,3,4-tetrahydroisoquinoline ( N-[ 11C] 7) and 1-(biphenyl-4-yl)methyl-6-[ 11C]methoxy-7-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline ( O-[ 11C] 7); and 2-(biphenyl-4-yl)- N-(3,4-dimethoxy-phenethyl)- N-[ 11C]methyl-ethanamine ( N-[ 11C] 10) and 2-(biphenyl-4-yl)- N-(3-methoxy-4-[ 11C]methoxy-phenethyl)- N-methyl-ethanamine ( O-[ 11C] 10), have been synthesized as new potential positron emission tomography (PET) glioma tumor imaging agents, either by O-[ 11C]methylation or by N-[ 11C]methylation of the appropriate precursors using [ 11C]CH 3OTf and isolated either by a simplified solid-phase extraction (SPE) purification procedure or by HPLC method in 30–55% radiochemical yields decay corrected to EOB, 15–25 min overall synthesis time, and 4.0–6.0 Ci/μmol specific activity at EOB.
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