6-[18F]fluoro-L-DOPA is a radiotracer widely used in the diagnosis of range diseases, including neuro-oncology, endocrinology, and Parkinson’s disease. To meet rapidly growing clinical need for this radioactive compound, study reports an optimized radiosynthesis molecule, which proved to be highly reliable compatible with different types automated radiosynthesizers. Moreover, 6-[18F]fluoro-L-DO...

Introduction: [18F]-6-thia-14-fluoro-heptadecanoic acid 3b, a free fatty acid, has been used in myocardial PET imaging. In order to establish an automated synthesis module for routine production in the country, a study performed for optimization of the production conditions as well as making modifications. Methods: [18F] Benzyl-14-Fluoro-6-thia-heptadecanoate 2b was prepared in no-carrier...

Progression of Parkinson's disease symptoms is imperfectly correlated with positron emission tomography biomarkers for dopamine biosynthetic pathways. The radiopharmaceutical 6-[(18) F]fluoro-m-tyrosine is not a substrate for catechol-O-methyltransferase and therefore has a more favorable uptake-to-background ratio than 6-[(18) F]fluoro-L-dopa. The objective of this study was to evaluate 6-[(18...

An eight-step linear sequence for the preparation of two diastereomers an 8-fluoro-ABC-steroid building block was developed. Key step intramolecular Diels–Alder reaction intermediate o-quinodimethane formed from a benzocyclobutene substituted with 5-fluorohex-5-en-4-one chain. This side chain prepared 6-chlorohex-1-ene by bromofluorination, elimination HBr, Finkelstein and alkylation literature...

Fludarabine phosphate (2-Fluoro-ara-AMP) is a purine analogue approved for the clinical treatment of haematological malignancies. This antimetabolite has also shown 'in vitro' antiproliferative activity against experimental models of solid mammary tumor. In this perspective, we have determined the cytotoxic effects of 2-Fluoro-ara-AMP against two human breast cancer cell lines (the ER-positive ...

Protein in vitro inhibition of thymidylate synthase (5,10-methylenetetrahydrofolate:dUMP C-methyltransferase, EC 2.1.1.45) by 5-fluoro-2'-deoxyuridylate requires 5,10-methylenetetrahydrofolate. The cytoxicity of 5-fluoro-2'-deoxyuridine towards cultured L1210 mouse leukemia cells is reduced when intracellular reduced folates are depleted, either by limiting the source in media or by inhibition ...

5-Fluoro-2'-deoxyuridylate causes a rapid inactivation of thymidylate synthetase that is dependent upon prior complexation of the cofactor 5,10-methylenetetrahydrofolate. The enzyme-5-fluoro-2'-deoxyuridylate complex may be isolated on nitrocellulose membranes and is not disrupted by 6 M urea. Upon reaction of 5-fluoro-2'-deoxyuridylate with the enzyme in the presence of 5,10-methylenetetrahydr...

The metabolic pathway of 2-deoxy-2-fluoro-D-galactose (FDGal) in mice was studied by 19F NMR. Efficient accumulation of FDGal in liver was demonstrated by NMR, which is consistent with the results of Ishiwata et al. using radioactive 18FDGal. The new discovery is that this fluorinated hexose was converted to 2-deoxy-2-fluoro-D-glucose (FDG) through UDP-FDGal and UDP-FDG apparently by the action...

In the title mol-ecule, C23H18F2N2O3S, the pyrimidine ring is in a half-chair conformation and the 3-fluoro-phenyl group is in the axial position. The thia-zole ring (r.m.s. deviation = 0.0252 Å) forms dihedral angles of 84.8 (7) and 9.6 (7)° with the 3-fluoro-substituted and 4-fluoro-substituted benzene rings, respectively. In the crystal, weak C-H⋯F and C-H⋯O hydrogen bonds connect mol-ecules...