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Synthesis of 14 C‐labelled 6‐hydroxy‐5,7‐dimethyl‐2‐(methylamino)‐4‐(3‐pyridylmethyl)benzothiazole dihydrochloride ( 14 C‐E3040 dihydrochloride)
Author(s) -
Hibi Shigeki,
Numata Hirotoshi,
Okamoto Yasushi,
Takenaka Osamu,
Mishima Mannen
Publication year - 1995
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.2580360507
Subject(s) - chemistry , benzothiazole , thiourea , yield (engineering) , medicinal chemistry , dimethyl sulfate , nuclear chemistry , stereochemistry , organic chemistry , metallurgy , materials science
14 C‐Labelled 6‐hydroxy‐5,7‐dimethyl‐2‐(methylamino)‐4‐(3‐pyridylmethyl)‐benzothiazole dihydrochloride ( 14 C‐E3040 dihydrochloride), required for a study of the phrmacokinetic profile of E3040, a novel dual inhibitor of 5‐lipoxygenase and thromboxane A 2 synthetase, was synthesized in one step using [2‐ 14 C]‐1‐methyl‐2‐thiourea as the labelled starting material. 14 C‐E3040 dihydrochloride with a specific activity of 58.0mCi/mmol was prepared in 60% chemical yield(based on thiourea 2 ).