摘要 |
PROBLEM TO BE SOLVED: To readily produce anα,α-difluoro-α-hydroxy ester useful as a synthetic intermediate for fluorine-containing physiologically active substances by using a specific chemically stable compound which can easily be synthesized as a raw material. SOLUTION: A silyldifluoro ester represented by formula I (R<1> to R<3> are each an alkyl, an aryl, a halogen or an alkoxy; R<4> is an alkyl or an aryl) is reacted with an aldehyde represented by formula II (R<5> is an alkyl, an aralkyl or an aryl) in the presence of fluoride anions to produce a compound represented by formula III. The compound represented by formula I is readily obtained by treating a difluoro ester represented by formula IV with lithium diisopropylamide. The compound represented by formula I is used in an amount of preferably 1-10mol, especially preferably 1-3mol based on 1mol aldehyde represented by formula II. The reaction can be carried out at a low to a high temperatures of -10 to +100 deg.C, especially preferably -78 to +40 deg.C.
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