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  • Title: Synthesis of Am80 (tamibarotene) prodrug candidates, congeners and metabolites.
    Author: Muratake H, Amano Y, Toda T, Sugiyama K, Shudo K.
    Journal: Chem Pharm Bull (Tokyo); 2013; 61(8):846-52. PubMed ID: 23902867.
    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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