摘要 |
<P>PROBLEM TO BE SOLVED: To provide a practical method for producing an optically active convolutamydine derivative expected to have various kinds of bioactivities. Ž<P>SOLUTION: The method for producing the optically active convolutamydine derivative includes reacting isatins with a silyl enol ether in the presence of a transition metal complex having optically active ligands to produce an optically active carbonyl-ene product, and reacting the obtained optically active carbonyl-ene product with an electrophile (E<SP>+</SP>), wherein, the carbonyl-ene reaction of the isatins with the silyl enol ether by an asymmetric catalyst progresses well. The suitable asymmetric catalyst and the reaction condition providing the objective substance especially in good yield at high optical purity are also cleared. As a result, the product not containing hardly separable impurities, and having the high chemical purity can be obtained. The optically active carbonyl-ene product obtained here can be reacted with various kinds of the electrophiles and can suitably be utilized for the introduction to various kinds required for the structure activity correlation. Ž<P>COPYRIGHT: (C)2010,JPO&INPIT Ž
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