| 摘要 |
PROBLEM TO BE SOLVED: To obtain on high yield the subject compound useful as a medicine or an intermediate for synthesizing medicines, by reaction of fan optically active epoxide or optically active epoxide precursor with an excess amount of an aliphatic alcohol in the presence of a fluoride. SOLUTION: This compound is obtained by reaction of an optically active epoxide of formula I (R<1> to R<4> are each H, a halogen or the like)(pref. propylene oxide) or an optically active epoxide precursor of formula II (X is a group eliminable when reacted with the alcohol described below)(e.g. 2-chloroethanol) with an excess amount of an aliphatic alcohol (pref. methanol) in the presence of a fluoride (e.g. sodium fluoride) at 15-160 deg.C. In the above process, as necessary, addition of a weak base (e.g. sodium bicarbonate) as an acid trapping agent accelerates the reaction and also enables the amount of the fluoride to be used to be reduced. It is preferable that the amounts of the aliphatic alcohol, the fluoride and the trapping agent to be used are 1.5-10 equivalents, 0.001-10 equivalents and 1-3 equivalents based on the reaction substrate, respectively. |
