Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 20, Pages 4587-4592Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.08.053
Keywords
[C-11]PBB3; Tau tracer; Radiosynthesis; Positron emission tomography (PET); Alzheimer's disease (AD)
Categories
Funding
- Indiana State Department of Health - United States (ISDH) Indiana Spinal Cord & Brain Injury Fund in the United States [ISDH EDS-A70-2-079612]
- National Science Foundation (NSF) - United States Major Research Instrumentation Program (MRI) [CHE-0619254]
Ask authors/readers for more resources
The authentic standard PBB3 and its precursor N-desmethyl-PBB3 as well as TBS-protected N-desmethyl-PBB3 precursor for radiolabeling were synthesized from 5-bromo-2-nitropyridine, acrolein diethyl acetal, 6-methoxy-2-methylbenzothiazole, and diethylchlorophosphate with overall chemical yield 1% in six steps, 2% in five steps, and 1% in six steps, respectively. [C-11]PBB3 was prepared from either desmethyl-PBB3 or TBS-protected desmethyl-PBB3 with [C-11]CH3OTf through N-[C-11] methylation and isolated by HPLC combined with SPE in 20-25% and 15-20% radiochemical yield, respectively, based on [C-11]CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was > 99%, and the specific activity at EOB was 370-1110 GBq/mu mol with a total synthesis time of similar to 40-min from EOB. (C) 2015 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available