3,6-双羧甲基-4-氨基-6H-噻吩并[2,3-B]吡咯-2-羧酸的合成研究

目的设计并合成3,6-双羧甲基-4-氨基-6H-噻吩并2,3-B]吡咯-2-羧酸。方法以柠檬酸为起始原料,经氧化酯化、Gewald反应、氮取代、环合、水解、脱羧反应制备得到目标化合物。结果合成了目标化合物,并利用质谱和核磁数据确证了结构;HPLC归一化法测得质量分数为96.98%。目标化合物的总收率为2.7%。结论 3,6-双羧甲基-4-氨基-6H-噻吩并2,3-B]吡咯-2-羧酸的合成为雷奈酸锶中杂质的研究提供了方便。

Synthesis of 3,6-bis(carboxymethyl)-4-amino-6H-thieno[2,3-b] pyrrole-2-carboxylic acid

Objective To design and synthesize 3,6-bis(carboxymethyl)-4-amino-6H-thieno2,3-b] pyrrole-2-carboxylic acid. Methods Citric acid was used as starting material to synthesize the target compound by oxidation, esterification, Gewald reaction, N-substituted, cyclization, hydrolysis, and decarboxylic reactions. Results The target compound was synthesized and characterized by MS and NMR data. And the purity detected by HPLC was 96.98%. The total recovery of the synthetic route was 2.7%. Conclusion The synthesis of 3,6-bis(carboxymethyl)-4-amino-6H-thieno2,3-b]pyrrole-2-carboxylic acid provides convenience for the study of impurities in strontium ranelate.