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Synthesis of 14C-labelled 6-hydroxy-5,7-dimethyl-2-(methylamino)-4-(3-pyridylmethyl)benzothiazole dihydrochloride (14C-E3040 dihydrochloride)

✍ Scribed by Shigeki Hibi; Hirotoshi Numata; Yasushi Okamoto; Osamu Takenaka; Mannen Mishima

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
113 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

14C-Labelled 6-hydroxy-5,7-dimethyl-2-(methylamino)-4-(3-pyridylmethyl)benzothiazole dihydrochloride (14C-E3040 dihydrochloride), required for a study of the phrmacokinetic profile of E3040, a novel dual inhibitor of 5-lipoxygenase and thromboxane A2 synthetase, was synthesized in one step using [2-W]-1methyl-2-thiourea as the labelled starting material. 14C-E3040 dihydrochloride with a specific activity of 58.0mCi/mmol was prepared in 60% chemical yield(based on thiourea 2 ).

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