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Microwave-assisted organic synthesis (MAOS) is rapidly becoming recognized as a valuable tool for easing some of the bottlenecks in the drug discovery process. This article outlines the basic principles behind the technology and summarizes the areas in which microwave technology has made an impact, to date.
[N-methyl- 11 C]Vorozole, a high-affinity aromatase-binding radiotracer, was synthesized through N-methylation of the corresponding nor-vorozole derivative using [ 11 C]methyl iodide. [N-methyl- 11 C]Vorozole was obtained in 53-56% radiochemical yield based on [ 11 C]methyl iodide within 40 min of the end of radionuclide production. The final formulation...
[carbonyl- 11 C]Estramustine and [carbonyl- 11 C]estramustine phosphate were synthesized from [ 11 C]phosgene using a one pot procedure. [carbonyl- 11 C]Estramustine was obtained in 31-43% decay corrected yield based on radioactivity trapped in the reaction vessel. The product was obtained 25 min after the end of radionuclide production with a specific...
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