目的 設(shè)計(jì)并合成3,6-雙羧甲基-4-氨基-6H-噻吩并[2,3-B]吡咯-2-羧酸。方法 以檸檬酸為起始原料,經(jīng)氧化酯化、Gewald反應(yīng)、氮取代、環(huán)合、水解、脫羧反應(yīng)制備得到目標(biāo)化合物。結(jié)果 合成了目標(biāo)化合物,并利用質(zhì)譜和核磁數(shù)據(jù)確證了結(jié)構(gòu);HPLC歸一化法測(cè)得質(zhì)量分?jǐn)?shù)為96.98%。目標(biāo)化合物的總收率為2.7%。結(jié)論 3,6-雙羧甲基-4-氨基-6H-噻吩并[2,3-B]吡咯-2-羧酸的合成為雷奈酸鍶中雜質(zhì)的研究提供了方便。

Objective To design and synthesize 3,6-bis(carboxymethyl)-4-amino-6H-thieno[2,3-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-thieno[2,3-b]pyrrole-2-carboxylic acid provides convenience for the study of impurities in strontium ranelate.