A novel synthesis of sitagliptin based on a redox-active ester derived from the chiral pool is reported. The key step is an electrochemical nickel-catalyzed sp²-sp³ cross-coupling reaction using inexpensive nickel foam in an undivided cell. It was successfully applied to 21 examples in up to 88% yield. These sitagliptin-analogue precursors could potentially interact with the DPP4 enzyme. A full synthesis based on our new reaction pathway provided sitagliptin in an overall yield of 33%.

中文翻译：

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西格列汀前体的电化学合成

报道了一种基于手性池衍生的氧化还原活性酯的西他列汀的新合成方法。关键步骤是在未分割的电池中使用廉价的镍泡沫进行电化学镍催化的sp ² -sp ³交叉偶联反应。它已成功应用于 21 个实例，产率高达 88%。这些西格列汀类似物前体可能与 DPP4 酶相互作用。基于我们的新反应途径的全合成提供了西格列汀，总收率为 33%。