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Synthesis of the 11C-labelled β-adrenergic receptor ligands atenolol, metoprolol and propranolol

1989; Pergamon Press; Volume: 40; Issue: 7 Linguagem: Inglês

10.1016/0883-2889(89)90109-3

1878-1128

Gunnar Antoni, Johan Ulin, Bengt Långström,

Chemical Reactions and Isotopes

The 11C-labelled β-adrenergic receptor ligands atenolol 1, metoprolol 2 and propranolol 3 have been synthesized by an N-alkylation reaction using [2-11C]isopropyl iodide. The labelled isopropyl iodide was prepared in a one-pot reactor system from [11C]carbon dioxide and obtained in 40% radiochemical yield within 14 min reaction time. The total reaction times for compounds 1–3, counted from the start of the isopropyl iodide synthesis and including purification were 45–55 min. The products were obtained in 5–15% radiochemical yields and with radiochemical purities higher than 98%. The specific activity ranged from 0.4 to 4 GBq/μmol. In a typical experiment starting with 4 GBq around 75 MBq of product was obtained.