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为控制罗库溴铵产品中的有关物质,分别合成了欧洲药典5.4版所载罗库溴铵的5种有关物质——2β-(4-吗啉基)-16β-(1-吡咯烷基)-5α-雄甾烷-3α,17β-二醇(1)、2β-(4-吗啉基)-16β-(1-吡咯烷基)-5α-雄甾烷-3α,17β-二醇-17-乙酸酯(2)、1-[3α,17β-二羟基-2β-(4-吗啉基)-5α-雄甾烷-16β-基]-1-(2-丙烯基)吡咯烷鎓溴化物(3)、1-[3α,17β-双(乙酰氧基)-2β-(4-吗啉基)-5α-雄甾烷-16β-基]-1-(2-内烯基)吡咯烷鎓溴化物(4)和1-[3α,17β-双(乙酰氧基)-2β-(1-吡咯烷基)-5α-雄甾烷-16β-基]-1-(2-内烯基)吡咯烷鎓溴化物(5),并经~1H NMR、~(13)C NMR和MS等确证结构。
In order to control the related substances in rocuronium products, five related substances of rocuronium, such as 2β- (4-morpholinyl) -16β- (1-pyrrolidinyl ) -5α-androstane-3α, 17β-diol (1), 2β- (4-morpholinyl) -16β- (1-pyrrolidinyl) (2) 1- [3α, 17β-dihydroxy-2β- (4-morpholinyl) -5α-androstane-16β-yl] -1- (2-propenyl) (3), 1- [3α, 17β-bis (acetyloxy) -2β- (4-morpholinyl) -5α-androstane-16β-yl] -1- (4) and 1- [3α, 17β-bis (acetyloxy) -2β- (1-pyrrolidinyl) -5α-androstane-16β-yl] -1- -alkenyl) pyrrolidinium bromide (5). The structures were confirmed by ~ 1H NMR, ~ (13) C NMR and MS.