摘要
We report herein the synthesis of impurity B of Flumazenil via demethylation, benzyl protection, cyclization and debenzylation from 7-methoxyl-3,4-dihydro-4-methyl-2H-1,4-benzo-diazepine-2,5(1H)-dione. The structure of impurity B of Flurnazenil was confirmed by 1n N/V[R, 13C NMR and HRMS, and the overall yield was 29.3%. The finding will be helpful for optimizing the synthetic process and quality control of Flumazenil.
我们以7-甲氧基-4-甲基-3H-1,4-苯并二氮杂卓-2,5-(1H,4H)–二酮为原料,经脱甲基、苄基保护、环合和脱苄基反应合成了氟马西尼有关物质B。氟马西尼有关物质B结构经氢谱、碳谱和高分辨质谱确证,总收率为29.3%。该发现有助于合成工艺的优化和氟马西尼的质量控制。