Synthesis of a radiotracer for studying nicotinic acetylcholine receptors: (+/−)-exo-2-(2-[18F]fluoro-5-pyridyl)-7-azabicyclo[2.2.1]heptane
✍ Scribed by Andrew Horti; Hayden T. Ravert; Edythe D. London; Robert F. Dannals
- Publisher
- John Wiley and Sons
- Year
- 1996
- Tongue
- French
- Weight
- 585 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
The radiochemical synthesis of (+/-)-exo-2-(2-[18F]fluoro-5-pyridyl)-7azabicyclo[2.2. llheptane ([W'lI_) was accomplished by Kryptofixa 222 assisted nucleophilic no-carrier-added [18F]fluorination of (+/-)-exo-2-(2-bromo-5-pyridyl)-7-azabicyclo[2.2.1] heptane (h). The average radiochemical yield of the final product was 10% and the average specific activity was greater than >2000 mCVpmo1, calculated at end-ofsynthesis. The stable fluorine ligand ([19E71) was prepared by Kryptofixa 222 assisted nucleophilic fluorination of (+/-)-exo-2-(2bromo-5-pyridyl) -7methoxycarbonyl -7azabicyclo[2.2. llheptane (a) followed by acid deprotection.
📜 SIMILAR VOLUMES
2-exo-(2 0 -Fluoro-3 0 -(4-fluorophenyl)-pyridin-5 0 -yl)-7-azabicyclo[2.2.1]heptane (F 2 PhEP), a novel, epibatidine-based, a4b2-selective nicotinic acetylcholine receptor antagonist of low toxicity, as well as the corresponding N-Boc-protected chloro-and bromo derivatives as precursors for labelli