| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for producing a substituted quinoline from a substituted aniline, improving its positional selectivity and yield. SOLUTION: This method for synthesizing the substituted quinoline expressed by the general formula D is characterized by reacting a substituted aniline sulfonamide compound expressed by the general formula A (wherein, R1, R2 and R3 are each independently selected from a group consisting of H, OH, an alkoxy, an alkyl, an amino, an amide or a halogen: and R4 is an alkyl or a substituted benzene) with acrolein in an alcohol containing triethylamine to synthesize an aldehyde intermediate expressed by the general formula B, then cyclizing the above aldehyde intermediate in trifluoromethane sulfonic acid (TfOH) or under an acidic condition to obtain a dihydroxyquinoline expressed by the general formula C, and treating the obtained compound by MOH (wherein, M is Na or K) in DMSO.
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