| 摘要 |
PURPOSE: Provided is a preparation method of 3-hydroxyquinoline based compound, jineol, having high anticancer activity and its derivative with high yield. CONSTITUTION: A method for preparation of jineol represented by the formula(1) and its derivative is composed of the following steps: (a) conversion of 8-hydroxy or alkoxyquinoline-3-carboxamide compound of the formula(6) into 3-amino-8-hydroxy or alkoxyquinoline compound of the formula(7); (b) reaction of the 3-amino-8-hydroxy or alkoxyquinoline compound, to obtain 3-hydroxy-8-hydroxy or alkoxyquinoline compound of the formula(8); and (c) reaction of the 3-hydroxy- 8-hydroxy or alkoxyquinoline compound to obtain quinoline based compound of the formula(1) or its derivative, wherein R1 is hydrogen or C1-C6 low alkyl group; R2 is selected from the group consisting of hydrogen, C1-C4 lower alkyl group, C1-C4 lower alkyl group potentially including phenyl group potentially having 1-3 substituents, C1-C6 lower alkyl group having hydroxy, C1-C5 alkoxy, acyloxy group, C5-C7 cycloalkyl group having substituent, C2-C7 lower acyl group, C2-C4 lower acyl group potentially including phenyl group potentially having 1-3 substituent, C2-C7 lower acyl group shaving hydroxy and C1-C5 alkoxy and acyloxy group, and C5-C7 cycloalkylcarbonyl group having 1-3 substituent.
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