A new high-yield synthetic route to PET CB1 radioligands [11C]OMAR and its analogs |
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| Authors: | Gao Mingzhang Wang Min Zheng Qi-Huang |
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| Affiliation: | Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN 46202, USA. |
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| Abstract: | OMAR analogs reference standards and their corresponding desmethylated precursors were synthesized from substituted anilines either in 4 and 5 steps with 27-32% and 24-31% yield, or in 3 and 4 steps with 21-30% and 19-28% yield, respectively. [(11)C]OMAR and its analog radioligands were prepared from their desmethylated precursors with [(11)C]CH(3)OTf through O-[(11)C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 50-65% radiochemical yields based on [(11)C]CO(2) and decay corrected to end of bombardment (EOB), with 370-740 GBq/μmol specific activity at EOB. |
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