Latli, Bachir published the artcilePotent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 labeled with carbon-13 and carbon-14, Recommanded Product: (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, the publication is Journal of Labelled Compounds and Radiopharmaceuticals (2017), 60(9), 420-430, database is CAplus and MEDLINE.
(S)-6-(2-Hydroxy-2-methylpropyl)-3-((S)-1-(4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl)ethyl)-6-phenyl-1,3-oxazinan-2-one (I) and (4aR,9aS)-1-(1H-benzo[d]midazole-5-carbonyl)-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-b]pyridine-6-carbonitrile hydrochloride (II) are potent and selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 enzyme. These 2 drug candidates developed for the treatment of type-2 diabetes were prepared labeled with carbon-13 and carbon-14 to enable drug metabolism, pharmacokinetics, bioanal., and other studies. In the carbon-13 synthesis, benzoic-13C6 acid was converted in 7 steps and in 16% overall yield to [13C6]-I. Aniline-13C6 was converted in 7 steps to 1H-benzimidazole-1-2,3,4,5,6-13C6-5-carboxylic acid and then coupled to a tricyclic chiral indenopiperidine to afford [13C6]-II in 19% overall yield. The carbon-14 labeled I was prepared efficiently in 2 radioactive steps in 41% overall yield from an advanced intermediate using carbon-14 labeled Me magnesium iodide and Suzuki-Miyaura cross coupling via in situ boronate formation. As for the synthesis of [14C]-II, 1H-benzimidazole-5-carboxylic-14C acid was first prepared in 4 steps using potassium cyanide-14C, then coupled to the chiral indenopiperidine using amide bond formation conditions in 26% overall yield.
Journal of Labelled Compounds and Radiopharmaceuticals published new progress about 1351413-50-7. 1351413-50-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Pyridine,Boronic Acids,Boronic acid and ester, name is (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, and the molecular formula is C6H8BNO3, Recommanded Product: (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem