申请人:The Upjohn Company
公开号:US04142054A1
公开(公告)日:1979-02-27
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. A continuous process using a Scheibel column is disclosed. 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 an 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.
2-芳基-C.sub.3至C.sub.6-烷酸酯可以通过在有机溶剂中将芳基烷基酮的烯醚与三价铊盐反应来经济地制备。通过向其中加入过氧酸和锰、钌、钴、铱、铪、锇或铌的反应形式来氧化一价铊离子至三价状态,可以再生三价铊离子,这可以按顺序、连续或化学计量的程序进行。公开了使用Scheibel柱的连续过程。然后,酯中间体产品转化为相应的2-芳基-C.sub.3至C.sub.6-烷酸或其盐。所选择的芳基团使得生成的酸产品将是一种有用的化合物,如抗炎药、镇痛药和退热药或农业上有用的产品。通过这种方法可以制备的药物酸的例子包括布洛芬、氟比洛芬、非洛芬和萘普洛昔等。