盐酸西那卡塞有关物质的合成

Synthesis of the Related Substances of Cinacalcet Hydrochloride

为控制盐酸西那卡塞的质量,本研究合成了4 个有关物质,分别为(2E)-N-[(1R)-1-(1-萘基)乙基]-3-[3-(三氟甲基)-苯基]丙-2-烯-1-胺盐酸盐(有关物质A),N-[(R)-1-(1-萘基)乙基]-3-[-3-(三氟甲基)苯基]丙-1-胺-N-氧化物(有关物质B),(E)-1-(1-萘基)乙酮肟(有关物质C)和(R)-N-乙基-1-萘乙胺盐酸盐(有关物质D),其中有关物质A、C、 D 未见文献报道。这些有关物质的结构均经MS、1H NMR 和13C NMR 确证。

In order to control the quality of cinacalcet hydrochloride, four related substances:(2E)-N-[(1R)-(naphthalen-2-yl)ethyl]-3-[3-(trifluoromethyl)phenyl]prop-2-en-1-amine hydrochloride (related substance A), N-[(R)-1-(naphthalen-1-yl)ethyl]-3-[3-(trifluoromethyl)phenyl]prop-1-amine-N-oxide(related substance B),(E)-1-(naphthalen-1-yl)ethanone oxime (related substance C) and (R)-N-ethyl-1-(naphthalen-1-yl)ethanamine hydrochloride (related substance D) were syhthesized, among them, related substances A, C, and D have not yet been reported in literature. The structures of these related substances were confirmed by MS, 1H NMR and 13C NMR.