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Related Experiment Videos

11C-labeling of busulphan.

M Hassan1, J O Thorell, N Warne

  • 1Karolinska Pharmacy, Stockholm, Sweden.

International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes
|January 1, 1991
PubMed
Summary

This study details a four-step synthesis for carbon-11 labeled busulphan, an alkylating agent for leukemia. The radiolabeled compound was produced efficiently, achieving high radiochemical purity for potential diagnostic applications.

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Area of Science:

  • Radiochemistry
  • Organic Synthesis
  • Nuclear Medicine

Background:

  • Busulphan is an alkylating agent used in chronic myelocytic leukemia treatment.
  • Positron-emitting radionuclides like carbon-11 are valuable for medical imaging.
  • Development of radiolabeled drugs enhances diagnostic and therapeutic capabilities.

Purpose of the Study:

  • To develop a reliable synthetic method for producing carbon-11 labeled busulphan.
  • To optimize the radiolabeling process for efficiency and yield.
  • To assess the radiochemical purity and feasibility of [1-11C]busulphan for potential applications.

Main Methods:

  • A four-step synthesis starting from [11C]cyanide and 3-bromopropanol.
  • Key steps include nitrile hydrolysis, lactone isolation via solid-phase extraction, diol reduction, and dimesylation.
  • High-performance liquid chromatography (HPLC) was used for purification.

Main Results:

  • [1-11C]4-Hydroxybutyronitrile obtained in 60-70% yield.
  • [1-11C]gamma-butyrolactone achieved in 80-90% yield.
  • [1-11C]busulphan synthesized with 30-35% conversion, 4-7% decay-corrected isolated yield, and >99% radiochemical purity within 65-75 minutes.

Conclusions:

  • A feasible four-step synthesis for [1-11C]busulphan was established.
  • The method provides high radiochemical purity suitable for further investigation.
  • This radiolabeled busulphan holds potential for nuclear medicine applications.

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