2014 Apr 5;90C:181-186. doi: 10.1016/j.apradiso.2014.03.029. [Epub ahead of print]
Facile and high-yield synthesis of N-(4-diethylamino)benzyl-4-[11C]methoxy-N-(p-tolyl)benzenesulfonamide as a new potential PET selective CB2 radioligand.
Abstract
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).
Copyright © 2014 Elsevier Ltd. All rights reserved.
Copyright © 2014 Elsevier Ltd. All rights reserved.
KEYWORDS:
Cancer, Cannabinoid receptor 2 (CB2), N-(4-Diethylamino)benzyl-4-[(11)C]methoxy-N-(p-tolyl)benzenesulfonamide, Neurological disorders, Positron emission tomography (PET), Radiosynthesis
- PMID:
24768996
[PubMed – as supplied by publisher]
