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

✍ Scribed by Svend B. Jensen; Dirk Bender; Donald F. Smith; Jørgen Scheel-Krüger; Elsebet Ø. Nielsen; Gunnar M. Olsen; Dan Peters; Albert Gjedde

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
112 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

(±) 3‐(6‐Nitro‐2‐quinolinyl)‐[9‐methyl‐^11^C]‐3,9‐diazabicyclo‐[4.2.1]‐nonane ([^11^C‐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 [^11^C]CO~2~ yielded 800 MBq of radiolabelled [^11^C‐methyl]NS 4194 in a formulated solution. The synthesis of the precursor to [^11^C‐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.

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