Pony Yu, Renyuan published the artcileIron-catalysed tritiation of pharmaceuticals, COA of Formula: C4H6N2, the publication is Nature (London, United Kingdom) (2016), 529(7585), 195-199, database is CAplus and MEDLINE.
A thorough understanding of the pharmacokinetic and pharmacodynamic properties of a drug in animal models is a critical component of drug discovery and development. Such studies are performed in vivo and in vitro at various stages of the development process-ranging from preclin. absorption, distribution, metabolism and excretion (ADME) studies to late-stage human clin. trials-to elucidate a drug mol.’s metabolic profile and to assess its toxicity. Radiolabeled compounds, typically those that contain 14C or 3H isotopes, are one of the most powerful and widely deployed diagnostics for these studies. The introduction of radiolabels using synthetic chem. enables the direct tracing of the drug mol. without substantially altering its structure or function. The ubiquity of C-H bonds in drugs and the relative ease and low cost associated with tritium (3H) make it an ideal radioisotope with which to conduct ADME studies early in the drug development process. Here we describe an iron-catalyzed method for the direct 3H labeling of pharmaceuticals by hydrogen isotope exchange, using tritium gas as the source of the radioisotope. The site selectivity of the iron catalyst is orthogonal to currently used iridium catalysts and allows isotopic labeling of complementary positions in drug mols., providing a new diagnostic tool in drug development.
Nature (London, United Kingdom) published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, COA of Formula: C4H6N2.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics