A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)...A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)-3-[(1R)-tert-butyldimethylsilyloxyethyl]-4-acetoxy-2-azetidi-none(4AA)upon thionocarboxlic acid.The intermediates and the target product were characterized by 1HNMR,IR,elementary analysis and MS.展开更多
4-羟基-L-脯氨酸、半胱胺盐酸为反应材料,经过一系列的氨基保护、氧化、缩合反应,得到Teneligliptin的关键中间体(2S)-4-氧代-2-(3-噻唑烷基羰基)-1-吡咯烷羧酸叔丁酯,收率可达73.8%。开发了一种全新的合成方式,在氧化阶段进行了改进和...4-羟基-L-脯氨酸、半胱胺盐酸为反应材料,经过一系列的氨基保护、氧化、缩合反应,得到Teneligliptin的关键中间体(2S)-4-氧代-2-(3-噻唑烷基羰基)-1-吡咯烷羧酸叔丁酯,收率可达73.8%。开发了一种全新的合成方式,在氧化阶段进行了改进和创新,对其质量进行控制,整个路线对环境几乎没有污染,并且通过1 H NMR和ESI-MS确认了设备的结构。展开更多
文摘A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)-3-[(1R)-tert-butyldimethylsilyloxyethyl]-4-acetoxy-2-azetidi-none(4AA)upon thionocarboxlic acid.The intermediates and the target product were characterized by 1HNMR,IR,elementary analysis and MS.
文摘4-羟基-L-脯氨酸、半胱胺盐酸为反应材料,经过一系列的氨基保护、氧化、缩合反应,得到Teneligliptin的关键中间体(2S)-4-氧代-2-(3-噻唑烷基羰基)-1-吡咯烷羧酸叔丁酯,收率可达73.8%。开发了一种全新的合成方式,在氧化阶段进行了改进和创新,对其质量进行控制,整个路线对环境几乎没有污染,并且通过1 H NMR和ESI-MS确认了设备的结构。