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

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

doi:10.1002/jlcr.542

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

Svend B. Jensen, Dirk Bender, Donald F. Smith, Jørgen Scheel-Krüger, Elsebet Nielsen, Gunnar M. Olsen, Dan Peters, Albert Gjedde

Research output: Contribution to journal › Article › peer-review

5 Scopus citations

Abstract

(±) 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.

Original language	English (US)
Pages (from-to)	181-189
Number of pages	9
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	45
Issue number	3
DOIs	https://doi.org/10.1002/jlcr.542
State	Published - Mar 15 2002
Externally published	Yes

Keywords

C
PET
Radiolabelling
Selective serotonin reuptake inhibitor

ASJC Scopus subject areas

Analytical Chemistry
Biochemistry
Radiology Nuclear Medicine and imaging
Drug Discovery
Spectroscopy
Organic Chemistry

Access to Document

10.1002/jlcr.542

Cite this

@article{d0de787a21034472a4adc7c460c17176,

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

abstract = "(±) 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.",

keywords = "C, PET, Radiolabelling, Selective serotonin reuptake inhibitor",

author = "Jensen, {Svend B.} and Dirk Bender and Smith, {Donald F.} and J{\o}rgen Scheel-Kr{\"u}ger and Elsebet Nielsen and Olsen, {Gunnar M.} and Dan Peters and Albert Gjedde",

year = "2002",

month = mar,

day = "15",

doi = "10.1002/jlcr.542",

language = "English (US)",

volume = "45",

pages = "181--189",

journal = "Journal of Labelled Compounds and Radiopharmaceuticals",

issn = "0362-4803",

publisher = "John Wiley and Sons Ltd",

number = "3",

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TY - JOUR

T1 - Synthesis of (±) 3-(6-nitro-2-quinolinyl)-[9-methyl-11C]-3,9-diazabicyclo-[4.2.1]- nonane ([11C-methyl]NS 4194)

AU - Jensen, Svend B.

AU - Bender, Dirk

AU - Smith, Donald F.

AU - Scheel-Krüger, Jørgen

AU - Nielsen, Elsebet

AU - Olsen, Gunnar M.

AU - Peters, Dan

AU - Gjedde, Albert

PY - 2002/3/15

Y1 - 2002/3/15

N2 - (±) 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.

AB - (±) 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.

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KW - Selective serotonin reuptake inhibitor

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