| 摘要 |
PURPOSE:To obtain a quinolinecarboaldehyde compound in high yield by oxidiz ing 2-cyclopropyl-4-(4-fluorophenyl)-3-hydroxymethylquinoline in the presence of a specific nitrosyl free radical derivative with a hypohalite. CONSTITUTION:2-Cyclopropyl-4-(4-fluorophenyl)quinoline-3-carboaldehyde is obtained by oxidizing 2-cyclopropyl-4-(4-fluorophenyl)-3-hydroxymethylquinoline. This oxidation reaction is carried out in the presence of a nitrosyl free radical derivative of formula I or formula II (X<1> and X<2> are each H, a halogen, OH, a 1-5C alkyl, a 5-6C cycloalkyl, a 1-5C alkoxy, a 1-10C acyloxy, etc., or X<1> and X<2> together form O; R<1> to R<4> are each a 1-5C alkyl; m is 0 to 1) with a hypohalite. Preferable examples of the nitrosyl free radical derivative include 2,2,6,6-tetramethylpiperidine-1-oxyl, etc. Further, potassium bromide or sodium bromide is preferably added into the reaction system. |
