We have investigated the use of cyclic sulfamidates as precursors to yield secondary amines as building blocks for subsequent reaction with carboxylic acids and acyl chlorides. The preparation of the protonated form of [F-18]-N-(2-fluoro-ethyl)-N-methylamine from the corresponding cyclic sulfamidate proceeded within a one pot two-step procedure (81 +/- 12%, n=10). The secondary amine reacted readily with acyl chlorides and/or carboxylic acids giving amides with yields ranging from 4 to 17% at the end of synthesis (182 +/- 12min). The new methodology provides a practical approach for the labelling of molecules where intramolecular cyclisation of precursors is favoured under typical radiofluorination conditions.
机构:
Harvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
Frullano, Luca
;
Catana, Ciprian
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Harvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
Catana, Ciprian
;
Benner, Thomas
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Harvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
Benner, Thomas
;
Sherry, A. Dean
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Univ Texas Dallas, Dept Chem, Dallas, TX 75230 USA
Adv Imaging Res Ctr, Dallas, TX USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
Sherry, A. Dean
;
Caravan, Peter
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Harvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
机构:
Univ Michigan, Dept Radiol, Ann Arbor, MI 48109 USAUniv Michigan, Dept Radiol, Ann Arbor, MI 48109 USA
Hoareau, Raphael
;
Scott, Peter J. H.
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Univ Michigan, Dept Radiol, Ann Arbor, MI 48109 USA
Univ Michigan, Interdept Program Med Chem, Ann Arbor, MI 48109 USAUniv Michigan, Dept Radiol, Ann Arbor, MI 48109 USA
机构:
Harvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
Frullano, Luca
;
Catana, Ciprian
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机构:
Harvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
Catana, Ciprian
;
Benner, Thomas
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机构:
Harvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
Benner, Thomas
;
Sherry, A. Dean
论文数: 0引用数: 0
h-index: 0
机构:
Univ Texas Dallas, Dept Chem, Dallas, TX 75230 USA
Adv Imaging Res Ctr, Dallas, TX USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
Sherry, A. Dean
;
Caravan, Peter
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机构:
Harvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USAHarvard Univ, Sch Med, Massachusetts Gen Hosp, AA Martinos Ctr Biomed Imaging, Charlestown, MA 02129 USA
机构:
Univ Michigan, Dept Radiol, Ann Arbor, MI 48109 USAUniv Michigan, Dept Radiol, Ann Arbor, MI 48109 USA
Hoareau, Raphael
;
Scott, Peter J. H.
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Univ Michigan, Dept Radiol, Ann Arbor, MI 48109 USA
Univ Michigan, Interdept Program Med Chem, Ann Arbor, MI 48109 USAUniv Michigan, Dept Radiol, Ann Arbor, MI 48109 USA