Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Synthesis of Am80 (Tamibarotene) Prodrug Candidates, Congeners and Metabolites
Hideaki Muratake Yohei AmanoTakahiro TodaKiyoshi SugiyamaKoichi Shudo
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2013 Volume 61 Issue 8 Pages 846-852

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Abstract
Compound 1 (IT-M-07000) was previously reported as a candidate prodrug of Am80 (Tamibarotene; used to treat acute promyelocytic leukemia), and shown to be efficiently metabolized to Am80 via β-oxidation. Here, we describe in detail the synthesis of 1, together with another tetradeuterated candidate prodrug, IT-YA-00616 (2), as well as two congeners, and several metabolic intermediates of 1 previously detected in mouse plasma.
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© 2013 The Pharmaceutical Society of Japan
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