| 摘要 |
NEW MATERIAL:A 3(R)-2-azetidinone derivative expressed by formula I (R<1> and R<2> are protecting groups of hydroxyl groups; R<3> is protecting group of amino group). EXAMPLE:(3R,4R)-1-Di-p-anisylmethyl-3-benzyloxy-4-[(R)-(1-tert- butyldimethylsilyloxy-1-phenyl)methyl]-2-azetidinone. USE:Useful as a synthetic intermediate for (2R,3S)-3-amino-4-cyclohexyl-2- hydroxybutyric acid derivatives useful as a raw material for producing peptidic compounds useful as a remedy for hypertension by human renin inhibitory activity. PREPARATION:An imine derivative expressed by formula II is reacted with a glycolic acid derivative expressed by formula III (X is Cl, Br or I) in the presence of a base to afford the objective compound expressed by formula I. |
