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Preparation of [18-F]haloperidol
Journal of Medicinal Chemistry
|May 1, 1975
Summary
Researchers developed a new method to synthesize [18F]haloperidol, a radiotracer. This efficient process yields high specific activity, crucial for positron emission tomography imaging applications.
Area of Science:
- Radiochemistry
- Nuclear Medicine
- Organic Synthesis
Background:
- Haloperidol is a typical antipsychotic drug.
- Radiolabeled haloperidol can be used as a tracer in Positron Emission Tomography (PET) imaging.
- Efficient synthesis of radiolabeled compounds is essential for clinical applications.
Purpose of the Study:
- To describe a novel procedure for the preparation of Fluorine-18 labeled haloperidol ([18F]haloperidol).
- To achieve high specific activity of [18F]haloperidol for improved PET imaging.
Main Methods:
- A Schiemann-type reaction was employed for the incorporation of Fluorine-18.
- Pyrolysis of the diazonium tetrafluoroborate salt of 4-[4-(p-chlorophenyl)-4-hydroxypiperidino]-4'-aminobutyrophenone was a key step.
- The synthesis was optimized for speed and yield.
Main Results:
- [18F]haloperidol was prepared in 140 minutes.
- Specific activities ranged from 4-5 muCi mg-1.
- The synthetic route proved effective for radiolabeling.
Conclusions:
- A rapid and efficient method for [18F]haloperidol preparation was established.
- The achieved specific activity is suitable for PET imaging.
- This procedure facilitates the availability of [18F]haloperidol for research and clinical use.