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合成了选择性雌激素受体调节剂巴多昔芬乙酸盐的5个有关物质,分别是:2-(4-羟基苯基)-3-甲基-1H-吲哚-5-酚(6),5-苄氧基-2-(4-羟基苯基)-3-甲基-1-[4-[2-(氮杂环庚烷-1-基)乙氧基]苄基]-1H-吲哚(7),3-[4-[2-(氮杂环庚烷-1-基)乙氧基]苄基]-2-(4-羟基苯基)-3-甲基-3H-吲哚-5-酚(8),1-(4-羟基苄基)-2-(4-羟基苯基)-3-甲基-1H-吲哚-5-酚(9),1-[4-[2-(氮杂环庚烷-1-基)乙氧基]苄基]-2-(4-羟基苯基)-3-甲基-1H-吲哚-5-酚-N-氧化物(10),并经1H NMR、13C NMR和MS确证结构,以作为巴多昔芬质量研究的参照物。
Five related substances of bazedoxifene acetate, a selective estrogen receptor modulator, were synthesized: 2- (4-hydroxyphenyl) -3-methyl-1H- 6) Synthesis of 5-benzyloxy-2- (4-hydroxyphenyl) -3-methyl- 1- [4- [2- (azepan-1-yl) ethoxy] benzyl] (7), 3- [4- [2- (azepan-1-yl) ethoxy] benzyl] -2- (4-hydroxyphenyl) (8), 1- (4-hydroxybenzyl) -2- (4-hydroxyphenyl) -3 -methyl- 1 H-indol-5-ol 1- [4- [2- (Azepan-1-yl) ethoxy] benzyl] -2- (4-hydroxyphenyl) -3-methyl-1H-indol-5-ol -N-oxide (10). The structure was confirmed by 1H NMR, 13C NMR and MS as a reference for the quality study of bazedoxifene.