罗匹尼罗中间体4-(2-苯甲酰氧乙基)-3-氯-1,3-二氢-2H-吲哚啉-2-酮的合成

Synthesis of 4-[2-(benzoyloxy)ethyl]-3-chloro-1,3-dihydro-2H-indolin-2-one,an Intermidiate of Ropinirole

以苯乙醇为原料,经分子内Friedel-Crafts烷基化反应合成了异色满,接着开环、成盐、水解得到苯甲酸-2-甲酰基苯乙基酯,再和硝基甲烷反应制备2-[2-(苯甲酰氧基)乙基]-β-硝基苯乙烯,最后通过Royer反应环合生成罗匹尼罗中间体4-(2-苯甲酰氧乙基)-3-氯-1,3-二氢-2H-吲哚啉-2-酮。产品经由薄层色谱、核磁共振谱、红外光谱分析,确为目的化合物,总收率为31.51%。

Isoehroman was synthesized from phenyl ethanol by inner molecular Friedel-Crafts alkylation reaction. The intermidiate of Ropinirole 4-[ 2-（benzoyloxy） ethyl ]-3-ehloro-1,3-dihydro-2H-indolin-2-one was prepared from isochroman by ring opening, salt formation, hydrolysis, nitrostyrene formation and Royer reaction. The target product was confirmed by the analysis of TLC,^1 H-NMR,IR.The total yield is 31.51%.