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Nucleoside Analogues For Positron Emission Tomography Imaging And To Study Radiation Mediated Generation Of Radicals From Azides, Maria E. De Cabrera
Nucleoside Analogues For Positron Emission Tomography Imaging And To Study Radiation Mediated Generation Of Radicals From Azides, Maria E. De Cabrera
FIU Electronic Theses and Dissertations
Gemcitabine is a potent anticancer cytidine analogue used to treat solid tumors. Its efficacy is diminished by rapid deamination to a toxic uridine derivative by cytidine deaminase. To overcome this limitation and add radioactive nuclei (18F or 68Ga) for PET imaging, I synthesized two 4-N-alkylgemcitabine analogues i) bearing β-keto tosylate moiety for subsequent 18F-fluorination and ii) having SCN-Bn-NOTA chelator to complex 68Ga. The first was synthesized by replacement of tosylamide in 4-N-tosylgemcitabine with 1-amino-10-undecene, followed by elaboration of terminal alkene through dihydroxylation, regioselective tosylation and oxidation. Subsequent fluorination using KF in …