RESUMO
Positron (ß(+)) emission tomography (PET) is a powerful, noninvasive tool for the in vivo, three-dimensional imaging of physiological structures and biochemical pathways. The continued growth of PET imaging relies on a corresponding increase in access to radiopharmaceuticals (biologically active molecules labeled with short-lived radionuclides such as fluorine-18). This unique need to incorporate the short-lived fluorine-18 atom (t1/2 = 109.77 min) as late in the synthetic pathway as possible has made development of methodologies that enable rapid and efficient late stage fluorination an area of research within its own right. In this review we describe strategies for radiolabeling with fluorine-18, including classical fluorine-18 radiochemistry and emerging techniques for late stage fluorination reactions, as well as labeling technologies such as microfluidics and solid-phase radiochemistry. The utility of fluorine-18 labeled radiopharmaceuticals is showcased through recent applications of PET imaging in the healthcare, personalized medicine and drug discovery settings.
Assuntos
Desenho de Fármacos , Radioisótopos de Flúor/química , Halogenação , Compostos Radiofarmacêuticos/química , Animais , Humanos , Tomografia por Emissão de Pósitrons , RadioquímicaRESUMO
Synthesis of the BCD ring system of cortistatin A has been accomplished in 9 steps and 30% overall yield starting from commercially available 2-methylcyclopent-2-enone. Key transformations include the addition of cyclopropenyllithium 16 to aldehyde 15, an intramolecular cyclopropene-furan [2 + 4] cycloaddition leading to epimers 18/19, and a subsequent cyclopropylcarbinyl rearrangement to afford 24.
