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邻氟苯乙酮经溴取代得2-溴代邻氟苯乙酮,经丙二腈取代、酸化闭环得2-氯-5-(2-氟苯基)-1H-吡咯-3-腈,经脱氯、镍催化氢化得5-(2-氟苯基)吡咯-3-甲醛,与吡啶-3-磺酰氯发生亲核取代反应生成5-(2-氟苯基)-1-(吡啶-3-磺酰基)-1H-吡咯-3-甲醛,与甲胺盐酸盐经还原氨化后与富马酸成盐得可逆性质子泵抑制剂富马酸沃诺拉赞,总收率25.5%(以邻氟苯乙酮计),纯度99.8%。
O-fluoro-fluoroacetophenone is substituted by bromine to give 2-bromo-o-fluoroacetophenone, which is substituted by malononitrile to form 2-chloro-5- After dechlorination and catalytic hydrogenation of nickel to give 5- (2-fluorophenyl) pyrrole-3-carbaldehyde, nucleophilic displacement reaction with pyridine-3-sulfonyl chloride gives 5- -3-sulfonyl) -1H-pyrrole-3-carbaldehyde with methylamine hydrochloride and reductive amination with fumaric acid to give a reversible proton pump inhibitor furaxonolazan, the total yield 25.5% (o-fluoroacetophenone), purity of 99.8%.