【摘要】 以3-氨基-2-羧基吡嗪为原料,经酯化反应、溴代反应生成化合物3,再经重氮化反应、氨解反应、氯代反应生成6,最后经苯环氟代反应、氰基水解反应、羟基取代反应即一锅煮反应合成法匹拉韦,总收率为26%。本文对酯化反应、溴代反应、氨解反应等反应过程中的反应条件等进行了优化;同时,其关键中间体3、6采用重结晶法纯化;最后3步反应采用一锅法完成,简化了操作。更多还原

【Abstract】 A preparation method of favipiravir was investigated,started from 3-aminopyrazine-2-carboxylicacid and subjected to esterification and bromination with NBS,compound 3 was synthesized. The brominated product was diazotized,aminated to obtain 6 which was suffered from fluorination,hydrolysis and hydroxyl substitution reaction namely one-pot reaction to afford favipiravir with an overall yield of about 22. 3%. Reaction conditions on esterification,bromination and so on were optimized. Additionally,pure key intermediates 3 and 6 were obtained via recrystallization from optimized solvents.Meanwhile,the last three steps were completed in one-pot procedure which simplified the operation.更多还原