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目的优化3-氨基-6-甲氧基噻吩并[2,3-b]喹啉-2-羧酸甲酯的合成工艺。方法以对甲氧基乙酰苯胺为原料,经过构建喹啉环、氰基化、硫化、构建噻吩环4步反应制备目标化合物,并优化各步反应条件。结果与结论目标化合物的结构经1H-NMR、13C-NMR和ESI-MS谱确证,总收率为67.3%(以对甲氧基乙酰苯胺计),优化后的工艺路线具有收率高、操作简单、污染低、适合大量制备等优点。
Aim To optimize the synthesis of 3-amino-6-methoxythieno [2,3-b] quinoline-2-carboxylic acid methyl ester. Methods Starting from p-methoxyacetanilide, the target compound was prepared through the four steps of quinoline ring, cyanation, sulfidation and thiophene ring construction, and the reaction conditions were optimized. Results and Conclusions The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR and ESI-MS spectra. The overall yield was 67.3% (based on p-methoxyacetanilide). The optimized route was characterized by high yield, Simple, low pollution, suitable for a large number of preparation and so on.