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Synthesis of 1‐(2‐ethoxyethyl)‐2‐(4‐methyl‐1‐homopiperazinyl)‐[2‐ 14 C]benzimidazole difumarate([ 14 C]KB‐2413)
Author(s) -
Awata Norio,
Satomi Osamu
Publication year - 1987
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.2580240314
Subject(s) - chemistry , benzimidazole , urea , radiosynthesis , yield (engineering) , isotope dilution , nuclear chemistry , radiochemistry , medicinal chemistry , organic chemistry , chromatography , mass spectrometry , in vivo , materials science , microbiology and biotechnology , metallurgy , biology
1‐(2‐Ethoxyethyl)‐2‐(4‐methyl‐1‐homopiperazinyl)‐[2‐ 14 C]‐benzimidazole difumarate ([ 14 C]KB‐2413), a new antihistaminic agent, was prepared from labelled urea. The synthetic intermediate, 1‐(2‐Ethoxyethyl)benzimidazolone, obtained in good yield by the condensation of N‐(2‐ethoxyethyl)‐o‐pheynylenediamine with [ 14 C]urea, was chlorinated with phosphorus oxychloride and followed by the reaction with N‐methylhomopiperazine to give the base of [ 14 C]KB‐2413. It was then converted to the difumarate, which was obtained in an overall radiochemical yield of 74% starting from [ 14 C] urea. The specific activity was 54.4 mCi/mmol and its radiochemical purity was 98.0% in reverse isotope dilution analysis.