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3-碘苯酚与1,2-二溴乙烷反应得3-碘-1-(2-溴代乙氧基)苯(4);另用丙二醇经二氧化锰氧化、与乙氧甲酰基亚甲基三苯膦经Wittig反应、羟基溴代得5-溴-2-戊烯酸乙酯(7)。用4和7在乙酸钯/三苯膦/降冰片烯作用下,与丙烯酸乙酯经C-H活化和分子内Heck反应得雷美替胺关键中间体2-[6,7-二氢-1H-茚并[5,4-b]呋喃-8(2H)-亚基]乙酸乙酯,总收率约51%。
3-iodophenol reacted with 1,2-dibromoethane to give 3-iodo-1- (2-bromoethoxy) benzene (4); another propylene glycol by manganese dioxide oxidation, Methyl triphenylphosphine by Wittig reaction, hydroxy brominated 5-bromo-2-pentenoate (7). Using 4 and 7 in the presence of palladium acetate / triphenylphosphine / norbornene reacted with ethyl acrylate via CH activation and intramolecular Heck reaction, the key intermediate of 2- (6,7-dihydro-1H- Indeno [5,4-b] furan-8 (2H) -ylidene] acetate in about 51% overall yield.