摘要 |
PROBLEM TO BE SOLVED: To provide an industrial method for production by which a dihydroxycoumarin derivative that is a useful synthetic intermediate for esculetins known to have cholesterol lowering, vascular reinforcing and antioxidizing actions can safely be produced in good yield without taking out a synthetic intermediate by using a readily industrially synthesizable raw material available in a large amount. SOLUTION: Alkoxyacrylic acids or 3, 3-dialkoxypropionic acids are reacted with a thionyl halide in the presence of a catalyst to synthesize alkoxyacryloyl halides or 3, 3-dialkoxypropionyl halides. The resultant compounds without being isolated are refluxed in the presence of an organic solvent under heating and a phenol derivative is added while removing a produced gas. Thereby, an aryl alkoxyacrylate derivative is synthesized. A strong acid is then added and reacted with the reaction solution as it is without isolating the aryl alkoxyacrylate derivative. As a result, the dihydroxycoumarin derivative can be produced in good yield. COPYRIGHT: (C)2004,JPO
|