Design of silicon-based misonidazole analogues and 18F-radiolabelling

Biocompatibility of Thermally Hydrocarbonized Porous Silicon Nanoparticles and their Biodistribution in Rats

“…All reagents and 1ϫ HBSS buffer were purchased from Sigma-Aldrich, except for absolute ethanol (Etax Aa, Ն 99.7 vol-%, Altia Corporation) and polyethylene glycol-15-hydroxystearate solubilizer (Solutol HS 15, BASF SE). Fluorine-18 was produced in a 18 O(p,n) 18 36,37 The solution was heated at 120°C for 15 min. Radiolabeled nanoparticles were purified with sequential washes in absolute ethanol, ultrapure water, and 1ϫ HBSS, pH ϭ 7.4.…”

Silicon-[18F]Fluorine Radiochemistry: Basics, Applications and Challenges

“…This high lipophilicity can result in a dramatically altered in vivo biodistribution of the labeled substances, especially in the case of small molecules. Thus, examples for small molecules containing organo-silicon building blocks for the introduction of 18 F are rare, but some approaches have been described recently [46][47][48].…”

“…One example is the preparation of 18 F-labeled silicon-based nitromidazoles ( Figure 15) that were designed as possible alternatives to the clinically relevant tracer [ 18 F]FMISO and intended for hypoxia-imaging [46]. The radiosynthesis of these compounds-bearing methyl, iso-propyl-, phenyl-and naphthyl-moieties in order to stabilize the Si- 18 F-bond-started from the corresponding alkoxy-silanes and gave good 18 F-incorporation yields at elevated temperatures of 75 °C for 20 min, but a final HPLC purification of the tracers was necessary.…”

Facile and Efficient Synthesis of [18F]Fluoromisonidazole Using Novel 2-Nitroimidazole Derivatives

“…1,14 Therefore, nitroimidazole derivatives with 18 F are used to quantify hypoxia through PET. [15][16][17][18] Among the derivatives, [ is widely known and studied by many medical groups. 14,[19][20][21][22][23] We were interested in developing a useful method for the synthesis of [ 18 F]FMISO for higher overall synthetic yield along with a higher radio synthetic yield.…”