Synthesis of (±) 3‐(6‐nitro‐2‐quinolinyl)‐[9‐methyl‐11C]‐3,9‐diazabicyclo‐[4.2.1]‐nonane ([11C‐methyl]NS 4194)

(±) 3‐(6‐Nitro‐2‐quinolinyl)‐9‐methyl‐¹¹C]‐3,9‐diazabicyclo‐4.2.1]‐nonane (¹¹C‐methyl]NS 4194), a selective serotonin reuptake inhibitor (SSRI), was synthesised within 35 min after end of bombardment with a radiochemical purity >98%. It had a decay‐corrected radiochemical yield of 7% after preparative HPLC, and a specific radioactivity around 37 GBq/μmol (EOS). A typical production starting with 40 GBq ¹¹C]CO₂ yielded 800 MBq of radiolabelled ¹¹C‐methyl]NS 4194 in a formulated solution. The synthesis of the precursor to ¹¹C‐methyl]NS 4194, (±) 9‐H‐3‐6‐nitro‐(2‐quinolinyl)]‐3,9‐diazabicyclo‐4.2.1]‐nonane, as well as the unlabelled analogue (±) 9‐methyl 3‐6‐nitro‐(2‐quinolinyl)]‐3,9‐diazabicyclo‐4.2.1]‐nonane (NS 4194), are also described. Copyright © 2002 John Wiley & Sons, Ltd.