210366-13-5Relevant academic research and scientific papers
Synthesis and iron chelating properties of hydroxypyridinone and hydroxypyranone hexadentate ligands
Zhou, Tao,Kong, Xiao-Le,Hider, Robert C.
, p. 3459 - 3466 (2019)
Chelation therapy has become an important therapeutic approach for some diseases. In attempt to identify clinically useful chelators, four hexadentate ligands were synthesized by conjugating the corresponding bidentate ligands (3-hydroxypyridin-4-one (3,4-HOPO), 3-hydroxypyridin-2-one (3,2-HOPO), 1-hydroxypyridin-2-one (1,2-HOPO), and 3-hydroxypyran-4-one) each with a free amino group to a tripodal acid. Their pKa values and affinities for iron(iii) were investigated. The pFe3+ values of the hexadentate pyridinones 1 (3,4-HOPO), 3 (3,2-HOPO) and 4 (1,2-HOPO), and the pyranone 2 was found to follow the sequence 1 > 4 ? 3 > 2, which is different to the pFe3+ value sequence of the corresponding bidentate forms (3,4-HOPO ? 3,2-HOPO > 1,2-HOPO > 3-hydroxypyranone). Hexadentate 3,4-HOPOs and 1,2-HOPOs have the greatest potential as iron scavenging agents.
Synthesis of 3,4,3 LI 1,2 HOPO labelled with 14C
Burgada,Bailly,Noel,Gomis,Valleix,Ansoborlo,Henge-Napoli,Paquet,Gourmelon
, p. 13 - 19 (2001)
3,4,3 LI 1,2 HOPO 1 or LIHOPO (1,5,10,14-tetra (1-hydroxy-2-pyridone-6-oyl)-1,5,10,14-tetraazatetradecane.) is a decorporation agent used against actinides. It was synthesised labelled with carbon 14 with a view to metabolism studies. [6,9-14C]-LIHOPO 2 was obtained in two radioactive steps through a very convenient synthesis in 50% radioactive yield from commercially available [1,4-14C]-spermine, hydrochloride and 1-benzyloxy-6-oxo-1,6-dihydropyridine-2-carbonyl chloride 7. The synthesis of 7 is also described.
MACROCYCLIC CHELATES AND USES THEREOF
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Page/Page column 51, (2021/07/17)
The present disclosure relates to macrocyclic chelates including a macrocyclic chelating moiety of a metal complex thereof, a bifunctional linker, and a therapeutic or targeting moiety. Also disclosed are methods for preparation of the same, and use thereof.
Ring-closing metathesis for the synthesis of heteroaromatics: evaluating routes to pyridines and pyridazines
Donohoe, Timothy J.,Bower, John F.,Basutto, José A.,Fishlock, Lisa P.,Procopiou, Panayiotis A.,Callens, Cedric K.A.
experimental part, p. 8969 - 8980 (2009/12/26)
Ring-closing olefin metathesis (RCM) has been applied to the efficient synthesis of densely and diversely substituted pyridine and pyridazine frameworks. Routes to suitable metathesis precursors have been investigated and the scope of the metathesis step has been probed. The metathesis products function as precursors to the target heteroaromatic structures via elimination of a suitable leaving group, which also facilitates earlier steps by serving as a protecting group at nitrogen. Further functionalisation of the metathesis products is possible both prior to and after aromatisation. The net result is a powerful strategy for the de novo synthesis of highly substituted heteroaromatic scaffolds.
