176967-62-7Relevant academic research and scientific papers
Utility of azetidinium methanesulfonates for radiosynthesis of 3-[ 18F]fluoropropyl amines
Kiesewetter, Dale O.,Eckelman, William C.
, p. 953 - 969 (2007/10/03)
3-Methanesulfonyloxypropyl tertiary amines were observed to cyclize to form azetidinium methanesulfonate moieties. Heat-induced cyclization of 3-methanesulfonyloxypropyl amines was utilized for preparation of azetidinium methanesulfonates. The azetidinium methanesulfonates were found to incorporate radioactive [18F]fluoride (decay-corrected yields > 60%) efficiently, resulting in an efficient synthesis of 3-[18F] fluoropropyl tertiary amines. Copyright
Synthesis of 1-(trans-[123I]Iodopropen-2-yl)-4- (4-cyanophenoxymethyl)piperidine: A selective sigma receptor radioligand for SPECT
Waterhouse,Collier,O'Brien
, p. 215 - 226 (2007/10/03)
1-(trans-[123I]Iodopropen-2-yl)-4-(4-cyanophenoxymethyl)piperidine has been prepared as a novel sigma receptor ligand for SPECT. This ligand was round to be selective in vitro for the sigma receptor site (Ki(σ) = 21.7 nM) when tested in a variety of neuroreceptor binding assays. The lipophilicity or this ligand (log P7.5 = 3.36) is appropriate for good brain uptake and relatively low non-specific binding. Radioiodination was accomplished using classical electrophilic iododestannylation methods and Specific activity of the purified product was >2100 mCi/μmole. Radiochemical yields were 60-80% EOS and radiochemical purities were >99%. The average time of synthesis and purification was 35 minutes.
