2,6-Pyridinedimethanol(cas: 1195-59-1) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.Synthetic Route of C7H9NO2
Synthetic Route of C7H9NO2In 2019 ,《Functionally Versatile and Highly Stable Chelator for 111In and 177Lu: Proof-of-Principle Prostate-Specific Membrane Antigen Targeting》 appeared in Bioconjugate Chemistry. The author of the article were Li, Lily; Jaraquemada-Pelaez, Maria de Guadalupe; Kuo, Hsiou-Ting; Merkens, Helen; Choudhary, Neha; Gitschtaler, Katrin; Jermilova, Una; Colpo, Nadine; Uribe-Munoz, Carlos; Radchenko, Valery; Schaffer, Paul; Lin, Kuo-Shyan; Benard, Francois; Orvig, Chris. The article conveys some information:
Here, we present the synthesis and characterization of a new potentially nonadentate chelator, H4pypa and its bifunctional analog tBu4pypa-C7-NHS conjugated to PSMA (prostate-specific membrane antigen) – targeting peptidomimetic (Glu-urea-Lys). H4pypa is very functionally versatile and biol. stable. Compared to the conventional chelators (e.g. DOTA, DTPA), H4pypa has outstanding affinities for both 111In (EC, t1/2 ∼2.8 d) and 177Lu (β-,γ t1/2∼6.64 d). Its radiolabeled complexes were achieved at >98% radiochem. yield, RT within 10 min, at ligand concentration as low as 10-6 M, with excellent stability in human serum over at least 5-7 days (<1% transchelation). The thermodn. stabilities of the [M(pypa)]- complexes (M3+ = In3+, Lu3+, La3+) were dependent on the ionic radii, where the smaller In3+ has the highest pM value (30.5), followed by Lu3+ (22.6) and La3+ (19.9). All pM values are remarkably higher than those with DOTA, DTPA, H4octapa, H4octox and H4neunpa. Moreover, the facile and versatile bifunctionalization enabled by the p-OH group in the central pyridyl bridge of the pypa scaffold (compound 14) allows incorporation of a variety of linkers for bioconjugation through easy nucleophilic substitution. In this work, an alkyl linker was selected to couple H4pypa to a PSMA-targeting pharmacophore, proving that the bioconjugation sacrifices neither the tumor-targeting nor the chelation properties. The biodistribution profiles of 111In- and 177Lu-labeled tracers are different, but promising, with the 177Lu analog particularly outstanding. In addition to this study using 2,6-Pyridinedimethanol, there are many other studies that have used 2,6-Pyridinedimethanol(cas: 1195-59-1Synthetic Route of C7H9NO2) was used in this study.
2,6-Pyridinedimethanol(cas: 1195-59-1) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.Synthetic Route of C7H9NO2
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