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A general 11C-labeling approach enabled by fluoride-mediated desilylation of organosilanes.
Qu, Wenchao; Hu, Bao; Babich, John W; Waterhouse, Nicole; Dooley, Marybeth; Ponnala, Shashikanth; Urgiles, Julie.
Afiliación
  • Qu W; Citigroup Biomedical Imaging Center, Weill Cornell Medicine, New York, NY, USA. Wenchao.qu@stonybrookmedicine.edu.
  • Hu B; Division of Radiopharmaceutical Sciences, Department of Radiology, Weill Cornell Medicine, New York, NY, USA. Wenchao.qu@stonybrookmedicine.edu.
  • Babich JW; Department of Psychiatry, Stony Brook University, Stony Brook, NY, USA. Wenchao.qu@stonybrookmedicine.edu.
  • Waterhouse N; Citigroup Biomedical Imaging Center, Weill Cornell Medicine, New York, NY, USA.
  • Dooley M; Division of Radiopharmaceutical Sciences, Department of Radiology, Weill Cornell Medicine, New York, NY, USA.
  • Ponnala S; Department of Psychiatry, Stony Brook University, Stony Brook, NY, USA.
  • Urgiles J; Citigroup Biomedical Imaging Center, Weill Cornell Medicine, New York, NY, USA.
Nat Commun ; 11(1): 1736, 2020 04 08.
Article en En | MEDLINE | ID: mdl-32269227
Carbon-11 (11C) is one of the most ideal positron emitters for labeling bioactive molecules for molecular imaging studies. The lack of convenient and fast incorporation methods to introduce 11C into organic molecules often hampers the use of this radioisotope. Here, a fluoride-mediated desilylation (FMDS) 11C-labeling approach is reported. This method relies on thermodynamically favored Si-F bond formation to generate a carbanion, therefore enabling the highly efficient and speedy incorporation of [11C]CO2 and [11C]CH3I into molecules with diversified structures. It provides facile and rapid access to 11C-labeled compounds with carbon-11 attached at various hybridized carbons as well as oxygen, sulfur and nitrogen atoms with broad functional group tolerance. The exemplified syntheses of several biologically and clinically important radiotracers illustrates the potentials of this methodology.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Radioisótopos de Carbono / Compuestos de Organosilicio / Fluoruros Idioma: En Revista: Nat Commun Asunto de la revista: BIOLOGIA / CIENCIA Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Radioisótopos de Carbono / Compuestos de Organosilicio / Fluoruros Idioma: En Revista: Nat Commun Asunto de la revista: BIOLOGIA / CIENCIA Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido