【摘要】 3,4-二氟苯胺在三乙胺存在下与二硫化碳生成芳基取代的二硫代氨基甲酸后与氯甲酸乙酯反应得到3,4-二氟苯基异硫氰酸酯,先后与由丙二酸二乙酯在无机碱中成的盐和氯甲基甲醚反应后加热环合,得到氟喹诺酮类抗菌剂普卢利沙星的中间体6,7-二氟-4-羟基-2-甲氧甲硫基-3-喹啉羧酸乙酯,总收率85.7%。更多还原

【Abstract】 Ethyl 6,7-difluoro-4-hydroxy-2-[(methoxymethyl)thio]quinoline- 3-carboxylate, a key intermediate ofprulifloxacin, was synthesized by treatment of 3,4-difluoroaniline with carbon disulfide in the presence of triethylamine andthen reacted with ethyl chloroformate to give 3,4-difluorophenylisothiocyanate, which reacted successively with diethylmalonate in the presence of KOH and chloromethyl methyl ether and then cyclization with an overall yield of 85.7%.更多还原