4.7 Article

A simple, rapid procedure for nucleophilic radiosynthesis of aliphatic [F-18]trifluoromethyl groups

Journal

CHEMICAL COMMUNICATIONS
Volume 47, Issue 43, Pages 11873-11875

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c1cc15342k

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Funding

  1. Medical Research Council [G0001354B, G1000183B] Funding Source: researchfish
  2. MRC [G0900903, G9439390, G0600986] Funding Source: UKRI
  3. Medical Research Council [G0600986, G0900903, G9439390, G0001354] Funding Source: Medline

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A procedure for the radiosynthesis of aliphatic [F-18] trifluoromethyl groups by reacting 1,1-difluorovinyl precursors with [(18) F] fluoride ions, resulting in the equivalent of direct nucleophilic addition of H[F-18] F, has been developed. A variety of F-18-labelled model compounds were then obtained and two potential [F-18] radiotracers were synthesised by a two step process starting from 1,1-difluorovin-2- yl 4-toluenesulfonate. The method is widely applicable for the synthesis of novel radiotracers in high radiochemical yields and good specific activity.

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