| 摘要 |
The invention pertains to a process for preparing (1-substituted benzyl)-3-(hydroxy-carbonyl aryl) condensed pyrazoles or (1-substituted benzyl)-3-(hydroxymethyl aryl) condensed pyrazoles comprising the steps of: (a) reacting compound I and compound II, or compound III and compound IV, to produce compound V, which is a substituted aryl ketone, as follows: <IMAGE> +TR <IMAGE> wherein Ar2 and At3 can be, independently, <IMAGE> R1 is H, C1-3 alkyl, or X (halogen), R3 is H, C1-3 alkyl, X (halogen), or -OR radical, and R is H or C1-3 alkyl; the process comprising the following steps of: R2 represents CH2OR, H, COOR, C1-3 alkyl, or X (halogen); (b) reacting the compound V with a hydrazine compound to form a hydrazone compound; (c) reacting the hydrazone compound compound with trifluoride etherate (BF3.Et2O) to form a 1-(substituted benzyl) 3-(substituted aryl) condensed pyraxzole, which is represented by the following formula of hydrolyzed or reduced to form corresponding carboxylic acids or alcohols.
|
