1171249-41-4

Upstream product

• 5292-43-3 bromoacetic acid tert-butyl ester 
• 140-28-3 N,N'-Dibenzylethylenediamine 
• 100-52-7 benzaldehyde 

Relevant academic research and scientific papers

Equilibrium, Kinetic and Structural Properties of Gallium(III) and Some Divalent Metal Complexes Formed with the New DATAm and DATA5m Ligands

The development of 68Ge/68Ga generators has made the positron-emitting 68Ga isotope widely accessible and raised interest in new chelate complexes of Ga3+. The hexadentate 1,4-di(acetate)-6-methyl[amino(methyl)acetate]perhydro-1,4-diazepane (DATAm) ligand and its bifunctional analogue, 1,4-di(acetate)-6-pentanoic acid[amino(methyl)acetate]perhydro-1,4-diazepane (DATA5m), rapidly form complexes with 68Ga in high radiochemical yield. The stability constants of DATAm and DATA5m complexes formed with Ga3+, Zn2+, Cu2+, Mn2+ and Ca2+ have been determined by using pH potentiometry, spectrophotometry (Cu2+) and 1H and 71Ga NMR spectroscopy (Ga3+). The stability constants of Ga(DATAm) and Ga(DATA5m) complexes are slightly higher than those of Ga(AAZTA). The species distribution calculations indicated the predominance of Ga(L)OH mixed-hydroxo complexes at physiological pH. The 1H and 71Ga NMR spectroscopy studies provided information about the coordinated functional groups of ligands and on the kinetics of exchange between the Ga(L) and Ga(L)OH complexes. The transmetalation reactions between the Ga(L) complexes and Cu2+ citrate (6?-assisted dissociation of the Ga(L)OH species. At pH 7.4 and 25 °C, the half-lives of the dissociation of Ga(DATAm), Ga(DATA5m) and Ga(AAZTA) were 11, 44 and 24 h, respectively. Similar half-lives have been obtained for the ligand-exchange reactions between the Ga(L)OH complexes and transferrin. The equilibrium and kinetic data indicate that the Ga(DATA5m) complex is a good 68Ga-based radiodiagnostic candidate.

Polyazamacrocycles based on a tetraaminoacetate moiety and a (poly)pyridine intracyclic unit: Direct synthesis and application to the photosensitization of Eu(III) and Tb(III) ions in aqueous solutions

A series of five new 15-, 18- or 21-membered polyazamacrocycles (L 1-L5) based on a pyridine, bipyridine or terpyridine unit and a triethylenetetraminetetraacetic acid (TTTA) skeleton is described. In ligands L4 and L

Hybrid chelator-based PSMA radiopharmaceuticals: Translational approach

(1) Background: Prostate-specific membrane antigen (PSMA) has been extensively studied in the last decade. It became a promising biological target in the diagnosis and therapy of PSMAexpressing cancer diseases. Although there are several radiolabeled PSMA

H4octapa: An acyclic chelator for 111In radiopharmaceuticals

This preliminary investigation of the octadentate acyclic chelator H 4octapa (N4O4) with 111In/ 115In3+ has demonstrated it to be an improvement on the shortcomings of the current industry "gold standards" DOTA (N 4O4) and DTPA (N3O5). The ability of H4octapa to radiolabel quantitatively 111InCl3 at ambient temperature in 10 min with specific activities as high as 2.3 mCi/nmol (97.5% radiochemical yield) is presented. In vitro mouse serum stability assays have demonstrated the 111In complex of H 4octapa to have improved stability when compared to DOTA and DTPA over 24 h. Mouse biodistribution studies have shown that the radiometal complex [111In(octapa)]- has exceptionally high in vivo stability over 24 h with improved clearance and stability compared to [ 111In(DOTA)]-, demonstrated by lower uptake in the kidneys, liver, and spleen at 24 h. 1H/13C NMR studies of the [In(octapa)]- complex revealed a 7-coordinate solution structure, which forms a single isomer and exhibits no observable fluxional behavior at ambient temperature, an improvement to the multiple isomers formed by [In(DTPA)]2- and [In(DOTA)]- under the same conditions. Potentiometric titrations have determined the thermodynamic formation constant of the [In(octapa)]- complex to be log KML = 26.8(1). Through the same set of analyses, the [111/115In(decapa)] 2- complex was found to have nonoptimal stability, with H 5decapa (N5O5) being more suitable for larger metal ions due to its higher potential denticity (e.g., lanthanides and actinides). Our initial investigations have revealed the acyclic chelator H 4octapa to be a valuable alternative to the macrocycle DOTA for use with 111In, and a significant improvement to the acyclic chelator DTPA.

An efficient route to pyridine and 2,2'-bipyridine macrocycles incorporating a triethylenetetraminetetraacetic acid core as ligand for lanthanide ions

Two novel macrocyclic chelators L1 and L2 incorporating an intracyclic pyridine or 2,2'-bipyridine unit and a triethylenetetraminetetraacetic acid core (TTTA) were synthesized with the aim of forming lanthanide complexes suitable as