| 摘要 |
PURPOSE:To obtain the subject compound important as a synthetic intermediate for medicines such as a beta-lactam-based antimicrobial agent in good yield by directly reacting a azetidinone derivative used as a raw material with an alcohol or a thiol compound in the presence of a copper compound. CONSTITUTION:An azetidinone derivative of formula I [OR1 is protected OH; R2 is alkyl or (substituted)aromatic] is made to react with an alcohol compound or a thiol compound of formula II (X is O or S; R3 is alkyl, alkenyl, aralkyl or aryl) in the presence of a copper compound to provide the objective 4- substituted azetidinone derivative of formula III [e.g. (3R,4R)-3-[(R)-1-(tert.- butyldimethylsilyloxy)ethyl]-4-aryloxy-2-azetidinone]. As the copper compound, copper (I) oxide or copper (II) oxide is preferably used. This method is industrially advantages because reactional process is shortened. |
