| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for preparing an aminopropanediol derivative useful as an important synthetic intermediate for an HIV protease inhibitor by using hydroxyoxazolidinone. SOLUTION: A compound of formula I (R is a 1-6C lower alkyl, phenyl or the like; R<1> is a protective group; P is an amino protective group) is hydrolyzed in the presence of a base to provide the objective aminopropanediol derivative of formula II in the method for preparing the aminopropanediol derivative. The derivative of formula II can be obtained by hydrolyzing a compound of formula III in the presence of the base to provide a compound of formula IV and protecting the amino group of the compound of formula IV. The derivative of formula II can also be obtained by protecting both the hydroxy group and the amino group of 2-hydroxymethyloxazolidin-2-one of formula V, hydrolyzing or ring-opening the protected 2-hydroxymethyloxazolidin-2-one in the presence of the base, or protecting the hydroxy group thereof, hydrolyzing and ring- opening the hydroxy-protected compound in the presence of the base, and protecting the amino group of the product. |
