Carbon-14-And Carbon-13-Labeled Phosphoric Acid [2-4-(4-Cyanophenyl)-Thiazol-2-Yl]-(2,4-Difluorophenyl)-1-[1,2,4]Triazol -4-Yl-Methylpropoxymethyl] Monoester Dilysine Salt, A Prodrug Of Ravuconazole

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS(2011)

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摘要
4-Bromobenzoic acid [carboxyl-(14)C] and 4-(2-bromoacetyl) [Ar-(13)C(6)]benzonitrile were transformed into the title compounds containing [ring (14)C-thiazol-4-yl] and [Ar-(13)C(6)-benzonitrile]. (14)C-Ravuconazole was prepared in 37% yield and Purity >99%. (13)C(6)-Ravuconazole was made in 56% overall yield and Purity of >98%. Each labeled compound was converted by additional reaction steps to the corresponding labeled prodrug.
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关键词
antifungal agents, 14 alpha-demethylase, ravuconazole, prodrug, phosphoric acid dilysine salt
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