【摘要】 3-羟基丙腈与双乙烯酮反应后与间硝基苯甲醛和3-氨基巴豆酸甲酯经"一锅煮"反应制得中间体2,6-二甲基-4-(间硝基苯基)-1,4-二氢吡啶-5-羧酸甲酯-3-羧酸(4);4用奎尼丁拆分得(R)-4;(R)-4与(S)-N-苄基-3-羟基吡咯烷经酯化和成盐反应合成了盐酸巴尼地平,总收率12.7%,其结构经1H NMR,IR和ESI-MS确证。更多还原

【Abstract】 A key intermediate,2,6-dimethyl-4-( m-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid-5-carboxylate( 4),was prepared by reaction of 3-hydroxy-propionitril with diketene,then reacted with m-nitrobenzaldehyde and methyl 3-aminocrotonate.( R)-4 was obtained by resolution of 4 using quinidine as the resolution agent. Barnidipine hydrochloride in total yield of 12. 7% was synthesized by esterification of( R)-4 with( S)-N-benzyl-3-hydroxy-pyrrolidine,then salifying. The structure was confirmed by1 H NMR,IR and ESI-MS.更多还原