马来酸依那普利有关物质的合成

Synthesis of the Related Substances of Enalapril Maleate

为控制马来酸依那普利(1)的质量,合成了4个有关物质,分别为N-[(S)-1-乙氧羰基-3-苯丙基]-L-丙氨酸(B)、N-[(S)-1-羧基-3-苯丙基]-L-丙氨酰-L-脯氨酸(C)、4N-[(S)-1′-乙氧羰基-3′-苯丙基]-3S-甲基-2,5-二酮-6S-H-1,4-二氮杂双环[4,3,0]壬烷(D)和N-[(S)-1-乙氧羰基-3-环己基丙基]-L-丙氨酰-L-脯氨酸马来酸盐(H),其结构经1H NMR和MS(ESI)确证。

In order to control the quality of enalapril maleate(1),four related substances,namely(S)-2-(((S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoic acid hydrochloride(B),(S)-1-((S)-2-(((S)-1-carboxy-3-phenylpropyl)amino)propanoyl)pyrrolidine-2-carboxylic acid(C),(S)-ethyl-2-((3S,8aS)-3-methyl-1,4-dioxohexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl)-4-phenylbutanoate(D),(S)-1-((S)-2-(((S)-4-cyclohexyl-1-ethoxy-1-oxobutan-2-yl)amino)propanoyl)pyrrolidine-2-carboxylic acid maleate(H),were synthesized based on the synthetic process of 1,and the structures of these compounds were confirmed by 1H NMR and MS(ESI).