Solid-phase radiosynthesis of [11C]WAY 100635

Article abstract of DOI:10.1002/(SICI)1099-1344(199602)38:2<149::AID-JLCR824>3.0.CO;2-8

An efficient, fast and simple method is described for the radiosynthesis of the potent and selective 5-HT_1A antagonist [O-methyl- ¹¹C]-N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexane carboxamide ([¹¹C]WAY 100635). [¹¹C]Iodomethane was effectively trapped on a C₁₈ reverse-phase cartridge at ambient temperature where it reacted rapidly with the normethyl precursor, N-[2-[4-(2-hydroxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexane carboxamide. Following high performance liquid chromatography purification and formulation, [¹¹C]WAY 100635 was obtained in high radiochemical yields (40%, uncorrected from [¹¹C]Iiodomethane) in a synthesis time of 25 min with an average specific actvity of (at end-of-synthesis) 33 GBq/μmole (900 mCi/μmole).