Gao Mingzhang, Lola Christian M, Wang Min, Miller Kathy D, Sledge George W, Hutchins Gary D, Zheng Qi-Huang
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208 Indianapolis, IN 46202, USA.
Appl Radiat Isot. 2010 Oct;68(10):1950-8. doi: 10.1016/j.apradiso.2010.04.030. Epub 2010 May 5.
Carbon-11-labeled tricyclic necroptosis inhibitors were first designed and synthesized as new potential PET agents for imaging of tumor necrosis factor alpha (TNF-alpha). The target tracers were prepared by O-[(11)C]methylation of their corresponding precursors using [(11)C]CH(3)OTf under basic conditions and isolated by a simplified SPE method in 50-60% radiochemical yields based on [(11)C]CO(2) and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 15-20 min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 111-185 GBq/micromol.
碳-11标记的三环坏死性凋亡抑制剂最初被设计并合成为用于肿瘤坏死因子α(TNF-α)成像的新型潜在正电子发射断层显像(PET)剂。通过在碱性条件下使用[(11)C]CH(3)OTf对其相应前体进行O-[(11)C]甲基化来制备目标示踪剂,并通过简化的固相萃取(SPE)方法进行分离,基于[(11)C]CO(2)的放射性化学产率为50-60%,并校正衰变至轰击结束(EOB)。从EOB开始的总合成时间为15-20分钟,放射性化学纯度>99%,合成结束时(EOS)的比活度为111-185 GBq/μmol。