Synthesis and in vivo imaging of a 18F-labeled PARP1 inhibitor using a chemically orthogonal scavenger-assisted high-performance method

Angew Chem Int Ed Engl. 2011 Feb 18;50(8):1922-5. doi: 10.1002/anie.201006579. Epub 2011 Jan 21.


Pedal to the metal: Using inverse Diels-Alder catalyst free TCO/Tz cycloadditions, we were able to quickly and selectively generate an 18F-labeled AZD2281-derivative from multiple different scaffolds (A–E). Excess cold material was removed within minutes using a TCO scavenger resin. This protocol allows the parallel synthesis of a library of potential PET imaging agents in a short time, increasing the efficiency of lead compound detection. The novel PET probe was successfully tested in biological assays and its potency and targeted accumulation was confirmed in vivo.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cyclooctanes / chemistry
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Fluorine Radioisotopes / chemistry
  • Humans
  • Mice
  • Mice, Nude
  • Neoplasms / diagnosis
  • Phthalazines / chemistry
  • Piperazines / chemistry
  • Poly(ADP-ribose) Polymerase Inhibitors*
  • Poly(ADP-ribose) Polymerases / metabolism
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry


  • Cyclooctanes
  • Enzyme Inhibitors
  • Fluorine Radioisotopes
  • Phthalazines
  • Piperazines
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Radiopharmaceuticals
  • Poly(ADP-ribose) Polymerases
  • olaparib