Synthesis of meta-substituted [(18)F]3-fluoro-4-aminopyridine via direct radiofluorination of pyridine N-oxides.

Due to their electron-rich aromatic structure, nucleophilic (radio)fluorination of pyridines is challenging, especially at the meta position. In this paper, we describe the first example of direct fluorination of a pyridine N-oxide to produce a meta fluorinated pyridine. Specifically, fluorination of 3-bromo-4-nitropyridine N-oxide produced in several minutes 3-fluoro-4-nitropyridine N-oxide in moderate yield at room temperature. This intermediate compound was later converted to 3-fluoro-4-aminopyridine easily by catalytic hydrogenation. Furthermore, this approach was successfully applied for labeling with fluorine-18. The use of pyridine N-oxides for the preparation of fluoropyridines is unprecedented in the chemical literature and has the potential to offer a new way for the synthesis of these important structures in pharmaceuticals and radiopharmaceuticals.

Three-dimensional imaging characteristics of the HEAD PENN-PET scanner.

UNLABELLED: A volume-imaging PET scanner, without interplane septa, for brain imaging has been designed and built to achieve high performance, specifically in spatial resolution and sensitivity. The scanner is unique in its use of a single annular crystal of Nal(Tl), which allows a field of view (FOV) of 25.6 cm in both the transverse and axial directions. Data are reconstructed into an image matrix of 128(3) with (2 mm)3 voxels, using three-dimensional image reconstruction algorithms. METHODS: Point-source measurements are performed to determine spatial resolution over the scanner FOV, and cylindrical phantom distributions are used to determine the sensitivity, scatter fraction and counting rate performance of the system. A three-dimensional brain phantom and 18F-FDG patient studies are used to evaluate image quality with three-dimensional reconstruction algorithms. RESULTS: The system spatial resolution is measured to be 3.5 mm in both the transverse and axial directions, in the center of the FOV. The true sensitivity, using the standard NEMA phantom (6 liter), is 660 kcps/microCi/ml, after subtracting a scatter fraction of 34%. Due to deadtime effects, we measure a peak true counting rate, after scatter and randoms subtraction, of 100 kcps at 0.7 mCi for a smaller brain-sized (1.1 liter) phantom, and 70 kcps for a head-sized (2.5 liter) phantom at the same activity. A typical 18F-FDG clinical brain study requires only 2 mCi to achieve high statistics (100 million true events) with a scan time of 30 min. CONCLUSION: The HEAD PENN-PET scanner is based on a cost-effective design using Nal(Tl) and has been shown to achieve high performance for brain studies and pediatric whole-body studies. As a full-time three-dimensional imaging scanner with a very large axial acceptance angle, high sensitivity is achieved. The system becomes counting-rate limited as the activity is increased, but we achieve high image quality with a small injected dose. This is a significant advantage for clinical imaging, particularly for pediatric patients.

Triple energy window scatter correction technique in PET.

A practical triple energy window technique (TEW) is proposed, which is based on using the information in two lower energy windows and one single calibration, to estimate the scatter within the photopeak window. The technique is basically a conventional dual-window technique plus a modification factor, which can partially compensate object-distribution dependent scatters. The modification factor is a function of two lower scatter windows of both the calibration phantom and the actual object. In order to evaluate the technique, a Monte Carlo simulation program, which simulates the PENN-PET scanner geometry, was used. Different phantom activity distributions and phantom sizes were tested to simulate brain studies, including uniform and nonuniform distributions. The results indicate that the TEW technique works well for a wide range of activity distributions and object sizes. The comparisons between the TEW and dual window techniques show better quantitative accuracy for the TEW, especially for different phantom sizes. The technique is also applied to experimental data from a PENN-PET scanner to test its practicality.

Energy-based scatter correction for 3-D PET scanners using NaI(T1) detectors.

Earlier investigations with BGO positron emission tomography (PET) scanners showed that the scatter correction technique based on multiple acquisitions with different energy windows are problematic to implement because of the poor energy resolution of BGO (22%), particularly for whole-body studies. We believe that these methods are likely to work better with NaI(TI) because of the better energy resolution achievable with NaI(TI) detectors (10%). Therefore, we investigate two different choices for the energy window, a low-energy window (LEW) on the Compton spectrum at 400-450 keV, and a high-energy window (HEW) within the photopeak (lower threshold above 511 keV). The results obtained for our three-dimensional (3-D) (septa-less) whole-body scanners [axial field of view (FOV) of 12.8 cm and 25.6 cm] as well as for our 3-D brain scanner (axial FOV of 25.6 cm) show an accurate prediction of the scatter distribution for the estimation of trues method (ETM) using a HEW, leading to a significant reduction of the scatter contamination. The dual-energy window (DEW) technique using a LEW is shown to be intrinsically wrong; in particular, it fails for line source and bar phantom measurements. However, the method is able to produce good results for homogeneous activity distributions. Both methods are easy to implement, are fast, have a low noise propagation, and will be applicable to other PET scanners with good energy resolution and stability, such as hybrid NaI(TI) PET/SPECT dual-head cameras and future PET cameras with GSO or LSO scintillators.

Dedicated PET scanners for breast imaging.

We have used computer simulations to compare two designs for a PET scanner dedicated to breast imaging with a whole-body PET scanner. The new designs combine high spatial resolution, high sensitivity, and good energy resolution to detect small, low-contrast masses. The detectors are position sensitive NaI(Tl) scintillators. The first design is a ring scanner surrounding the breast and the second consists of two planar detectors placed on opposite sides of the breast. We have employed standard performance measures to compare the different designs: contrast, percentage standard deviation of the background, and signal-to-noise ratios of reconstructed images. The results of the simulations show that both of the proposed designs have better lesion detectability than a whole-body scanner. The results also show that contrast is higher in the ring breast system but that the noise is lower in the planar breast system. Overall, the ring system yields images with the best signal-to-noise ratios, although the planar system offers practical advantages for imaging the breast and axilla.

Current and future technological trends in positron emission tomography.

Current trends in positron emission tomography (PET) instrumentation are examined, with an emphasis on providing information suitable to the prospective PET user. Basic principles underlying PET are explained and information on performance measurements, techniques, and quantitation are given in order to allow the user to compare and contrast different types of PET scanners. These scanner designs are described. Specific examples are given and the combination of PET with other modalities is discussed.