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布洛芬(Ibuprofen)和萘普生(Naproxen)作为α-芳基丙酸类非甾体抗炎镇痛剂,在医疗上广泛使用。由于这类药物比传统的阿司匹林疗效高,副作用小,使人们对它们的需求量不断增长。然而在大规模工业生产这类药物时,却受到了反应条件、产物收率、中间体分离、特殊试剂的使用、环境保护、劳动防护等因素的限制,为此,人们一直在寻找既经济合理,又适于工业规模生产的合成途径。近年来,α-芳基丙酸类化合物的新的合成方法陆续在有关文献上报导,其中1,2-芳基重排转位方法引人注目,很有可能用于大规模工业化生产。
Ibuprofen and Naproxen are widely used medically as α-aryl propionic acid non-steroidal anti-inflammatory analgesics. Because these drugs have a higher therapeutic effect and less side effects than traditional aspirin, the demand for them is constantly increasing. However, in the large-scale industrial production of such drugs, they have been subject to the reaction conditions, product yield, intermediate separation, the use of special reagents, environmental protection, labor protection and other factors, people have been looking for both economic and reasonable , But also suitable for industrial-scale production of synthetic routes. In recent years, a new synthesis of α-arylpropionic compounds gradually reported in the literature, including 1,2-aryl rearrangement transposing method attracts attention, is likely to be used for large-scale industrial production.