一种新的高产量 PET CB1 放射性配体 [11C]OMAR 及其类似物的合成途径。
A new high-yield synthetic route to PET CB1 radioligands [11C]OMAR and its analogs.
机构信息
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
出版信息
Bioorg Med Chem Lett. 2012 Jun 1;22(11):3704-9. doi: 10.1016/j.bmcl.2012.04.030. Epub 2012 Apr 11.
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.
OMAR 类似物标准品及其对应的去甲基前体可由取代苯胺经 4 步或 5 步反应（收率分别为 27-32%和 24-31%）或 3 步或 4 步反应（收率分别为 21-30%和 19-28%）制得。[(11)C]OMAR 及其类似物放射性配体可由其去甲基前体与 [(11)C]CH(3)OTf 通过 O-[(11)C]甲基化反应制得，并采用 HPLC 结合固相萃取（SPE）进行分离，放射性化学产率为 50-65%，基于 [(11)C]CO2 和到轰击结束的校正（EOB），放射性比活度为 370-740GBq/μmol，在 EOB 时达到最大值。
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