申请人:The Upjohn Company
公开号:US04135051A1
公开(公告)日:1979-01-16
2-Aryl-C.sub.3 to C.sub.6 -alkanoate esters are prepared economically by reacting an enol ether of an aryl alkyl ketone with a trivalent thallium salt in an organic solvent. The trivalent thallium ions can be regenerated by adding a peracid and a reactive form of manganese, ruthenium, cobalt, iridium, hafnium, osmium or neobium to oxidize monovalent thallium ions to the trivalent state, in a sequential, continuous or stoichiometric procedure. The ester intermediate product is then converted to the corresponding 2-aryl-C.sub.3 - to C.sub.6 -alkanoic acid or salt thereof. The aryl group is selected so the resulting acid product will be a useful compound such as anti-inflammatory, analgesic and anti-pyretic drug or agriculturally useful product. Examples of drug acids which can be made by this process include ibuprofen, flurbiprofen, fenoprofen and naproxen and the like.
通过在有机溶剂中将芳基烷基酮的烯醇醚与三价铊盐反应,经济地制备2-芳基-C.sub.3至C.sub.6-烷酸酯。通过添加过氧酸和锰、钌、钴、铱、铪、锇或钽的反应性形式,将一价铊离子氧化为三价状态,以连续、连续或化学计量的程序再生三价铊离子。然后将酯中间体转化为相应的2-芳基-C.sub.3至C.sub.6-烷酸或其盐。选择芳基,使得所得的酸产品将是一种有用的化合物,例如抗炎、镇痛和退热药物或农业有用产品。通过这种方法可以制备的药物酸包括布洛芬、氟布洛芬、芬普罗芬和萘普生等。