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Synthesis of diethyl 4‐(benzothiazol‐[2‐ 14 C]‐2‐yl) benzylphosphonate ([ 14 C]KB‐944)
Author(s) -
Awata Norio,
Sato Akeshi
Publication year - 1983
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.2580200511
Subject(s) - chemistry , yield (engineering) , grignard reaction , diethyl carbonate , medicinal chemistry , barium carbonate , carbon 14 , barium , radiochemistry , nuclear chemistry , organic chemistry , reagent , raw material , materials science , physics , ethylene carbonate , electrode , quantum mechanics , electrolyte , metallurgy
Diethyl 4‐(benzothiazol‐[2‐ 14 C]‐2‐yl)benzylphosphonate ([ 14 C]KB‐944), a new calcium antagonist, was prepared from labelled carbon dioxide. The synthetic intermediate, [ 14 C]p‐toluic acid, obtained by the Grignard reaction was condensed with 2‐aminothiophenol, brominated with N‐bromosuccinimide, and followed by the Arbuzov reaction. [ 14 C]KB‐944, having the specific activity 52.7 mCi/mmol, was obtained in 36% overall yield from [ 14 C] barium carbonate and its radiochemical purity was 99.3% in reverse isotope dilution analysis.