| 摘要 |
PURPOSE:To obtain clebopride in high yield, by selectively rearranging and decomposing the 4-aminocarbonyl group of a reaction product of 4- aminocarbonyl-5-chloro-2-methoxybenzoic acid and 4-amino-1-benzylpiperidine. CONSTITUTION:A 1,4-dioxane solution of a compound of formula I (R is H or lower alkyl) or its reactive functional derivative at the lower ester is dripped to a 1,4-dioxane solution of the compound of formula II and triethylamine under cooling and the mixture is heated at 50-60 deg.C for 1-2hr under stirring to obtain the compound of formula III. A DMSO solution of the compound of formula III is dripped with an aqueous solution of 1.5 times equivalent to potassium hypobromite and 2-7 times equivalent of KOH under cooling and the mixture is heated at 50-80 deg.C for 1-3hr under stirring to obtain the objective compound of formula IV. The objective compound useful as a remedy for peptic ulcer can be economically produced on an industrial scale by the above process.
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