A Facile Synthetic Approach to Labeled 4-Acetoxy-2-(4-methylphenyl)benzothiazole

Noriyuki HORI; Norihiko SEKO; Goro TSUKAMOTO; Kohichiro YOSHINO

doi:10.1248/cpb.44.1248

Noriyuki HORI, Norihiko SEKO, Goro TSUKAMOTO, Kohichiro YOSHINO

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Keywords: 4-acetoxy-2-(4-methylphenyl)benzothiazole, cross-coupling reaction, isotopic label, Grignard reagent, zinc chloride

JOURNAL FREE ACCESS

1996 Volume 44 Issue 6 Pages 1248-1249

DOI https://doi.org/10.1248/cpb.44.1248

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Abstract

To study the pharmacokinetics and metabolism of 4-acetoxy-2-(4-methylphenyl)benzothiazole (KB-2683), which has potential immunomodulating activity, a practical preparation of labeled KB-2683 was needed. This paper describes an efficient method for the synthesis of ¹⁴C-labeled KB-2683 by means of procedures which include a metal-catalyzed cross-coupling reaction.

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