A new high-yield synthetic route to PET CB1 radioligands [C-11]OMAR and its analogs

作者：Gao Mingzhang; Wang Min; Zheng Qi Huang^*

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(11): 3704-3709.

DOI：10.1016/j.bmcl.2012.04.030

• [C-11]OMAR ([C-11]JHU75528)
• Cannabinoid receptor 1 (CB1)
• Radiosynthesis
• Automation
• Positron emission tomography (PET)
• Brain imaging

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. [C-11]OMAR and its analog radioligands were prepared from their desmethylated precursors with [C-11]CH3OTf through O-[C-11] methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 50-65% radiochemical yields based on [C-11]CO2 and decay corrected to end of bombardment (EOB), with 370-740 GBq/mu mol specific activity at EOB.

• 出版日期2012-6-1