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Radiolabeling of two 11 C‐labeled formylating agents and their application in the preparation of [ 11 C]benzimidazole
Author(s) -
Schou Magnus,
Halldin Christer
Publication year - 2012
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2972
Subject(s) - chemistry , benzimidazole , yield (engineering) , formic acid , carbon 14 , carbon 13 , carbon fibers , reducing agent , radiochemistry , nuclear chemistry , organic chemistry , materials science , physics , quantum mechanics , composite number , metallurgy , composite material
The radiolabeling of formyl groups with carbon‐11 has so far been awarded little attention in the literature. We report here the preparation of the methyl and trifluoroethyl esters of [ 11 C]formic acid and their use as 11 C‐formylating agents in the preparation of [ 11 C]benzimidazole. Methyl‐ethyl and trifluoroethyl [ 11 C]formates were obtained in 36–45% radiochemical yield using a two‐step two‐pot process starting from [ 11 C]carbon dioxide. The analytical radiochemical yield of [ 11 C]benzimidazole using each of these two 11 C‐formylating agents exceeded 96%. Given the high yields of the 11 C‐formylating agents as well as the high yield of [ 11 C]benzimidazole following their application, we expect these agents to find utility for a wider range of substrates.