Synthesis of a radiotracer for studying nicotinic acetylcholine receptors: 2-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[18F]A- 85380)

Article abstract of DOI:10.1002/(SICI)1099-1344(199804)41:4<309::AID-JLCR78>3.0.CO;2-I

The radiochemical synthesis of 2-[¹⁸F]fluoro-3-(2(S)- azetidinylmethoxy)pyridine (2-[¹⁸F]A-85380, [¹⁸F]1) was accomplished by Kryptofix 222 assisted nucleophilic no-carrier-added [¹⁸F]fluorination of 2-iodo-3-((1-tert-butoxycarbonyl-2(S)-azetidinyl)methoxy)pyridine, 2 followed by acidic deprotection. The average radiochemical yield was 10% and the average specific radioactivity was 1050 mCi/μmol, calculated at end-of- synthesis (EOS).