| 摘要 |
NEW MATERIAL:The isoindoline derivative of formula I (R<1> is H or lower alkyl; R<2> is H, lower alkyl or acyl). EXAMPLE:N-4-(isoindolyl-2-one)-salicylic acid. USE:A medicinal drug having especially high anti-inflammatory and antithrombotic activities as well as analgesic action and antipyretic action. PREPARATION:The compound of formula I can be produced economically in high yield, by (1) reacting the compound of formula II (R<3> is alcohol residue) with the compound of formula III in an alcohol solvent (e.g. methanol, ethanol, propanol, etc.) at room temperature or under heating to obtain the compound of formula IV, (2) cooling the reaction mixture solution on an ice bath without separating the produced compound from the solution and adding 1-3mol of sodium borohydride or potassium borohydride as a reducing agent based on 1mol of the compound of formula IV, and (3) carrying out the reaction of the components at room temperature for 0.5-10hr after the addition of the reducing agent.
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