Automated synthesis of 11C-acetoacetic acid, a key alternate brain fuel to glucose

Appl Radiat Isot. 2007 Aug;65(8):934-40. doi: 10.1016/j.apradiso.2007.03.015. Epub 2007 Mar 28.

Abstract

An automated, one-pot radio-synthesis module for the routine preparation of 1-[(11)C]acetoacetic acid has been developed. The enolate anion of acetone was reacted with [(11)C]CO(2) in tetrahydrofuran (THF), followed by hydrolysis and purification by ion-exchange chromatography. The total synthesis time was 18 min and radiochemical yield was 34% after decay correction. HPLC analysis showed < or =3% impurities while residual THF (< or =200 ppm) and ethanol (< or =500 ppm) were well under the tolerable limits for human studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetoacetates / analysis
  • Acetoacetates / chemical synthesis*
  • Acetoacetates / isolation & purification*
  • Acetoacetates / metabolism
  • Animals
  • Brain / metabolism
  • Carbon Radioisotopes / analysis
  • Carbon Radioisotopes / chemistry*
  • Carbon Radioisotopes / isolation & purification*
  • Carbon Radioisotopes / metabolism
  • Chromatography, Ion Exchange / instrumentation
  • Chromatography, Ion Exchange / methods*
  • Drug Contamination / prevention & control
  • Glucose / metabolism
  • Humans
  • Isotope Labeling / instrumentation
  • Isotope Labeling / methods*
  • Radiopharmaceuticals / analysis
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / isolation & purification
  • Radiopharmaceuticals / metabolism
  • Robotics / instrumentation
  • Robotics / methods*

Substances

  • Acetoacetates
  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • acetoacetic acid
  • Glucose