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为控制富马酸替诺福韦酯的质量,分别合成了美国药典32版收载的5种有关物质:(R)-[[2-[6-(异丙氧基甲酰胺基)-9H-嘌呤-9-基]-1-甲基乙氧基]甲基]膦酸双(异丙基氧基羰酰氧甲基)酯(有关物质A)、(R)-[[2-(6-氨基-9H-嘌呤-9-基)-1-甲基乙氧基]甲基]膦酸单(异丙基氧基羰酰氧甲基)酯(有关物质B)、(R)-[[2-(6-氨基-9H-嘌呤-9-基)-1-甲基乙氧基]甲基]膦酸(异丙基氧基羰酰氧甲基)(乙氧基羰酰氧甲基)酯(有关物质C)、(R)-[[2-(6-氨基-9H-嘌呤-9-基)-1-甲基乙氧基]甲基]膦酸(异丙基氧基羰酰氧甲基)(甲基)酯(有关物质D)、(R)-[[2-(6-氨基-9H-嘌呤-9-基)-1-甲基乙氧基]甲基]膦酸(异丙基氧基羰酰氧甲基)(异丙基)酯(有关物质E),并经1H NMR和ESI-MS等确证结构。
In order to control the quality of tenofovir disoproxil fumarate, five related substances contained in the 32 edition of the United States Pharmacopeia were synthesized: (R) - [[2- [6- (isopropoxycarboxamido) -9H 9-yl] -1-methylethoxy] methyl] phosphonic acid bis (isopropyloxycarbonyloxymethyl) ester (related substance A) 9-yl) -1 -methylethoxy] methyl] phosphonic acid mono (isopropyloxycarbonyloxymethyl) ester (related substance B), (R) - [[2- (6-Amino-9 H -purin-9-yl) - 1 -methylethoxy] methyl] phosphonic acid (isopropyloxycarbonyloxymethyl) (ethoxycarbonyloxy (R) - [[2- (6-amino-9H-purin-9-yl) - 1 -methylethoxy] methyl] phosphonic acid (isopropyloxy (R) - [[2- (6-amino-9H-purin-9-yl) -1-methylethoxy] methyl ] (Isopropyloxycarbonyloxymethyl) (isopropyl) phosphonate (related substance E), and the structures were confirmed by 1H NMR and ESI-MS.