Patent classifications
C07B59/005
OLIGONUCLEOTIDE-BASED THERAPEUTICS AND USES THEREOF
Described herein are compounds that are useful for delivering therapeutic, diagnostic, and imaging agents. Also described herein are pharmaceutical compositions containing such compounds and methods of using the compounds and compositions. Also described are processes for manufacture of the compounds and the compositions containing them.
FLUORINATION PROCESS
The present disclosure relates to processes for the fluorination of molecules. One aspect provides a process for incorporating a fluorine atom into a molecule, said process comprising converting a compound of formula X-SG into a compound of formula X-F, wherein G is an optionally substituted C.sub.1-C.sub.6 alkyl group, an optionally substituted aryl group, or an optionally substituted heteroaryl group, and X is an organic group; and wherein the SG group is attached to a secondary or tertiary carbon atom in the organic group X; said process comprising treating said compound of formula X-SG with (i) an activator compound selected from the group consisting of N-halosuccinimides, N-halobenzenesulfonimides, N-halobenzenesulfonamides, dialkylaminodihalosulfinium salts, heterocyclylaminodihalosulfinium salts, dialkylaminosulfur trihalides, XeF.sub.2, difluoroiodotoluene, di- and tri-bromoisocyanuric acids, bromine, chlorine, hypervalent iodine compounds with I.sub.2; and other sources of Br.sup.+, Cl.sup.+, F.sup.+, I.sup.+, bromonium, iodonium, or chloronium; and (ii) a source of fluoride. Uses of the process in the preparation of various fluorinated molecules as well as uses of certain compounds as intermediates in the processes of the present disclosure are also provided.
ONE-STEP KIT-BASED SYNTHESIS OF 2-DEOXY-2-[18F]FLUORO-D-SORBITOL
A self-contained kit and method for the on-demand synthesis of 2-deoxy-2-[.sup.18F]fluoro-D-sorbitol (.sup.18F-FDS) from commercially available 2-deoxy-2-[.sup.18F]fluoroglucose (.sup.18F-FDG) is disclosed.
METHODS AND MATERIALS FOR MAKING PET RADIOTRACERS
Embodiments of the present disclosure provide compositions comprising compounds useful to make radiotracers for positron emission tomography imaging, as well as methods for making and using these compositions.
Phosphoramidates for the treatment of hepatitis B virus
Disclosed are compounds to the treatment of infectious diseases and methods of treating such diseases. The compounds are derivatives of clevudine.