非奈利酮有关物质的合成

Synthesis of the Related Substances of Finerenone

为了更好对非奈利酮进行质量控制,合成了5个有关物质,分别是4-(4-氰基-2-甲氧基苯基)-6-乙基-2,8-二甲基-5-氧代-1,4,5,6-四氢-1,6-萘啶-3-甲酰胺(有关物质A)、4-(4-氰基-2-甲氧基苯基)-5-乙氧基-2,8-二甲基-1,6-萘啶(有关物质B)、3-羟基-4-(4-氰基-2-甲氧基苯基)-5-乙氧基-2,8-二甲基-1,6-萘啶(有关物质C)、4-(4-氨基甲酰基-2-甲氧基苯基)-5-乙氧基-2,8-二甲基-1,4-二氢-1,6-萘啶-3-甲酰胺(有关物质D)和4-(4-氰基-2-甲氧基苯基)-5-乙氧基-2,8-二甲基-1,6-萘啶-3-甲酰胺(有关物质E)。上述有关物质均经1H NMR、13C NMR和HRMS结构确证。

In order to control the quality of finerenone,this study synthesized five related substances,namely 4-(4-cyano-2-methoxyphenyl)-6-ethyl-2,8-dimethyl-5-oxy-1,4,5,6-tetrahydro-1,6-naphthyridin-3-carboxamide(related substance A),4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,6-naphthyridine(related substance B),3 hydroxy-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,6-naphthyridine(related substance C),4-(4-aminocarbonyl 2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carboxamide(related substance D),and 4-(4 cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,6-naphthyridin-3-carboxamide(related substance E).The chemical structures of these substances were confirmed by 1H NMR,13C NMR and HRMS.