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以4-硝基苯酚为原料,经乙酰化、硝基还原得4-乙酰氧基苯胺,与乙酰乙酸乙酯在溴化铟作用下反应,再在碳酸钾、乙酸钯及乙酸铜作用下闭环得5-乙酰氧基-2-甲基-1H-吲哚-3-羧酸乙酯,再经甲基化、溴代、苯硫酚取代和脱保护制得6-溴-5-羟基-1-甲基-2-苯硫甲基-1H-吲哚-3-羧酸乙酯,然后以氨基磺酸为酸试剂、水为溶剂,经Mannich反应得盐酸阿比朵尔,总收率45.4%(以4-硝基苯酚计)。
4-nitrophenol as raw material, acetylation, nitro reduction of 4-acetoxyaniline, and ethyl acetoacetate in the role of indium bromide reaction, and then in potassium carbonate, palladium acetate and copper acetate ring closed Ethyl 5-acetoxy-2-methyl-1H-indole-3-carboxylate, followed by methylation, bromination and thiophenol substitution and deprotection to obtain 6-bromo- 1-methyl-2-phenylthiomethyl-1H-indole-3-carboxylic acid ethyl ester, and then aminosulfonic acid as an acid reagent, water as a solvent, Mannich reaction of abiraterone hydrochloride, the total yield 45.4% (based on 4-nitrophenol).