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吲哚布芬(indobufen),化学名2-[4-(1-氧代-2-异吲哚啉基)苯基]丁酸(1),是一种新的抗凝药,于1984年8月在意大利首次上市。文献报道可由2-(4-氨基苯基)丁酸乙酯与苯甲醛,或2-溴甲基苄腈或2-(4-氨基苯基)丁酸(2)与邻苯二甲醛缩合制得。以上合成方法各有使用剧毒的光气或氰化亚铜,或耗用大量的溴的问题,均不适宜工业生产。本文采用邻苯二甲酸酐与2缩合,再经锌-乙酸还原即得产品,总收率达58％。此法在文献中未见报道,有反应步骤少、原料易得、操作简便的优点。所得产品的红外光谱、核磁共振、质谱与邻苯二甲醛与2缩合所得样品一致。
Indobufen, a chemical name 2- [4- (1-oxo-2-isoindolinyl) phenyl] butyric acid (1), is a new anticoagulant, August IPO in Italy for the first time. Reported in the literature can be ethyl 2- (4-aminophenyl) butyrate and benzaldehyde, or 2-bromomethyl benzonitrile or 2- (4-aminophenyl) butyric acid (2) condensation with phthalate formaldehyde Got it. The above synthesis methods each use highly toxic phosgene or cuprous cyanide, or consume a large amount of bromine, are not suitable for industrial production. In this paper, phthalic anhydride and 2 condensation, and then by zinc - acetic acid to obtain the product, the total yield of 58%. This method has not been reported in the literature, there are few reaction steps, raw materials are easy to obtain, easy to operate. The resulting product was characterized by infrared spectroscopy, nuclear magnetic resonance, mass spectrometry and ortho-phthalaldehyde in accordance with the sample obtained by condensation of 2.