The reference standard N-(4-diethylamino)benzyl-4-methoxy-N-(p-tolyl)benzenesulfonamide (3c) (CB2, Ki=0.5nM; CB1, Ki=1297nM; selectivity CB1/CB2=2594) and its corresponding precursor N-(4-diethylamino)benzyl-4-hydroxy-N-(p-tolyl)benzenesulfonamide (3d) were synthesized from 4-(diethylamino)benzaldehyde and p-toluidine in 3 steps with 75-84% overall chemical yield. The target tracer N-(4-diethylamino)benzyl-4-[11C]methoxy-N-(p-tolyl)benzenesulfonamide ([11C]3c) was synthesized from the phenol hydroxyl precursor by O-[11C]-methylation with [11C]CH3OTf, followed by HPLC combined with SPE purification in 40-50% decay corrected radiochemical yields with 370-740GBq/μmol specific activity at the end of bombardment (EOB).
- Cannabinoid receptor 2 (CB2)
- Neurological disorders
- Positron emission tomography (PET)
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