专利号:US-6140515-A 优先权日:1997-09-24 标题 :Process of making 3-aryloxy, 4-aryl furan-2-ones useful as inhibitors of COX-2 发明人:CHEN CHENG Y; TAN LUSHI; LARSEN ROBERT D 权利人:MERCK & CO INC 摘要:Described is a process of preparing 3-aryl, 4-aryloxy furan-5-ones which are useful as inhibitors of cyclooxygenase-2 (COX-2). Such compounds are useful as anti-inflammatory agents. The process is directed to an asymmetric synthesis which involves: a trisubstituted styrene derivative preparation via Horner-Wadsworth-Emmons reaction and subsequent one pot trifluoromethylation of the allylic alcohol; preparation of the alpha -hydroxyl ketone using Sharpless asymmetric dihydroxylation and Swern oxidation; the esterification of the alpha -hydroxyl ketone with the phenoxy acetic acid; and the Dieckman condensation of the resulting ester.
专利号:CN-108586399-B 优先权日:2018-07-03 标题 :Synthesis method of feloxicib