| 摘要 |
PROBLEM TO BE SOLVED: To efficiently produce anα,α'-aminoalcohol derivative that is useful as an intermediate for HIV protease inhibitor by starting with L-serine and passing via a novel oxazolinone intermediate. SOLUTION: A compound of formula I (R<1> is an alkyl) ms allowed to react with a halomagnesium dialkylamide in the presence of a haloacetic acid and magnesium chloride to form a compound of formula II. The product is reduced with sodium borohyciride or the like, then, the product is treated with a base such as potassium t-butoxide to form a compound of formula III. Further, the product is allowed to react with a compound of formula IV, then with a thiophenol, and the product is protected its amino group to give the objective compound of formula V (R<2> may be substituted with an alkyl, a heteroaryl or an aralkyl).
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