499237-86-4

Upstream product

• 100-39-0 benzyl bromide 
• 499237-85-3 3-(3-hydroxy-2-oxo-2H-pyridin-1-yl)-propionic acid ethyl ester 
• 627-32-7 1-iodopropan-3-ol 
• 94475-64-6 3-(benzyloxy)pyridin-2(1H)-one 
• 16867-04-2 dihydroxypyridine 

Downstream Products

• 1048636-37-8 3-(benzyloxy)-1-(3-chloropropyl)pyridin-2(1H)-one 
• 1286215-86-8 N,N-bis{3-[3-(benzyloxy)-2-oxopyridin-1(2H)-yl]propyl}-4-nitrobenzenesulfonamide 
• 499237-99-9 1-(3-azidopropyl)-3-benzyloxypyridin-2-one 
• 499238-00-5 3-[3-(benzyloxy)-2-oxopyridin-1(2H)-yl]propanamine 

Relevant academic research and scientific papers

Alpha-emitting complexes

The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.

A practical route for the preparation of 1,4,7-triazacyclononanyl diacetates with a hydroxypyridinonate pendant arm

The preparation of triazamacrocyclic hydroxypyridinonate (HOPO-TACN) derivatives as potential chelators for metals in biomedical applications was reported. The synthesis is based on a convergent synthetic approach, in which the key intermediate di-tert-butyl-2,2′-(1,4,7-triazonane-1,4-diyl) diacetate was coupled with a hydroxypyridinonate pendant arm. The method is suitable for rapid syntheses of metal chelator HOPO-TACNs of biomedical interest.

FLUORIDE-RELEASING COMPOSITIONS

Chelating monomers and fluoride-releasing compositions are disclosed that may be incorporated into dental composite restorative materials, dental bonding agents or other dental materials, to produce materials with high fluoride release rates, and high fluoride recharge capability. Such dental restorative materials may help reduce the level of dental caries in patients, particularly the level of caries occurring on the margins of the restorative materials.

New methodology for the preparation of 3-hydroxy-2-pyridinone (3,2-HOPO) chelators - Reaction of amines with a novel electrophilic 3,2-HOPO precursor

The preparation of the new electrophilic iminium ester mesylate salt 5 and its reaction with primary and secondary amines have been investigated. Aniline, t-butylamine, and secondary amines react with 5 via ring opening to give the corresponding HOPO derivatives in high yields. The usefulness of this methodology has been demonstrated by the preparation of two new di-HOPO derivatives 19 and 21. This method allows the introduction of the HOPO ligand onto a variety of amine platforms without the concomitant formation of an amide bond and provides access to HOPO chelators of increased water solubility.