Premium
Solid‐phase radiosynthesis of [ 11 C]WAY 100635
Author(s) -
Wilson Alan A.,
DaSilva Jean N.,
Houle Sylvain
Publication year - 1996
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199602)38:2<149::aid-jlcr824>3.0.co;2-8
Subject(s) - radiosynthesis , chemistry , cyclohexane , carboxamide , chemical synthesis , phase (matter) , nuclear chemistry , medicinal chemistry , stereochemistry , organic chemistry , in vivo , in vitro , biochemistry , microbiology and biotechnology , biology
An efficient, fast and simple method is described for the radiosynthesis of the potent and selective 5‐HT 1A antagonist [ O‐methyl ‐ 11 C]‐N‐[2‐[4‐(2‐methoxyphenyl)‐1‐piperazinyl]ethyl]‐N‐(2‐pyridinyl)cyclohexane carboxamide ([ 11 C]WAY 100635). [ 11 C]Iodomethane was effectively trapped on a C 18 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, [ 11 C]WAY 100635 was obtained in high radiochemical yields (40%, uncorrected from [ 11 C]Iiodomethane) in a synthesis time of 25 min with an average specific activity of (at end‐of‐synthesis) 33 GBq/μmole (900 mCi/μmole).