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Base-free process for the preparation of ketone intermediates usable for manufacture of nebivolol

机译:用于制备奈必洛尔的酮中间体的无碱制备方法

摘要

The invention relates to a process for the preparation of a ketone of a general formula 1 with X being Cl or Br, in particular with X being Cl, with Y being F, Cl, Br, I or H, in particular with Y being F, comprising the steps of: activation of a carboxylic acid by using a peptide coupling agent, coupling of the activated carboxylic acid with a malonic acid derivative providing a ²- ketoester precursor and converting the ² -ketoester precursor to the ketone of the general formula 1.
机译:本发明涉及制备通式1的酮的方法其中X是Cl或Br,特别是X是Cl,Y是F,Cl,Br,I或H,特别是Y是F,包括以下步骤:通过使用肽偶联剂活化羧酸,将活化的羧酸与丙二酸衍生物偶合,提供2-酮酸酯前体,并将2-酮酸酯前体转化为通式1的酮。

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