摘要 |
PURPOSE:To prepare the titled compound useful as a synthetic intermediate of bestatin, etc., with a simple operation, in high yield and optical purity, by oxidizing an optically active beta-aminoalcohol under specific condition. CONSTITUTION:The objective compound can be prepared by reacting the optically active beta-aminoalcohol of formula (R1 is amino-protecting group, etc.; R2 and R4 are H or alkyl; R3 is H, alkyl or aryl) with a sulfur trioxide complex in dimethyl sulfoxide in the presence of triethylamine for several minutes - ten-odd minutes. The sulfur trioxide complex is e.g. the complex of sulfur trioxide with pyridine, dioxane, DMF, etc. |