We have developed a TfOH-catalyzed, highly efficient protocol for the synthesis of biologically active β-acylamino ketones from aldehyde, ketone, and nitrile by avoiding the use of acetyl chloride. The reaction proceeds through a sequential aldol reaction followed by a nucleophilic attack of nitrile and hydrolysis of nitrile in one pot. The attractive features of this tandem process are mild reaction conditions, high atom economy, broad substrate scope with 51–87% yield, gram-scale reaction, and ease of operation.

中文翻译：

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TfOH 催化避免使用乙酰氯，一锅法轻松合成 β-酰氨基酮

我们开发了一种 TfOH 催化的高效方案，通过避免使用乙酰氯，从醛、酮和腈合成具有生物活性的 β-酰氨基酮。该反应通过连续的醇醛缩合反应，然后在一锅中进行腈的亲核攻击和腈的水解。这种串联工艺的吸引人的特点是反应条件温和、原子经济性高、底物范围广、产率51-87%、克级反应和易于操作。