| 摘要 |
PROBLEM TO BE SOLVED: To provide a practical method for producing an optically active fluorinated oxetane which can be an important pharmaceutical or agrochemical intermediate. SOLUTION: The method for producing the optically active fluorinated oxetane is provided, comprising: reacting a fluorinatedα-keto ester with an acyl alkenyl ether in the presence of a "transition metal complex having an optically active ligand". Specifically, this method is a catalytic asymmetrical synthetic method, and does not require a stoichiometric amount of a chiral source. In particular, by performing the reaction at high substrate concentration (using a small amount of a reaction solvent) or in the absence of a reaction solvent (in neat), the amount of an asymmetric catalyst used can be dramatically reduced. Further, the objective optically active fluorinated oxetane is obtained in a high yield with extremely high optical purity and also few impurities which are difficult to separate are contained therein, and thus, the product with high chemical purity is obtained. Therefore, the usefulness of this method is evident. COPYRIGHT: (C)2011,JPO&INPIT |
